N-(tetrazol-5-yl)- and n-(triazol-5-yl)arylcarboxamides and their use as herbicides

ABSTRACT

N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the formula (I) are described as herbicides. 
     
       
         
         
             
             
         
       
     
     In this formula (I), X, Y, Z and R represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B represent N and CY.

CROSS REFERENCE TO RELATED APPLICATIONS

This application claims priority to European Application number 10174893.7, filed Sep. 1, 2010, the contents of which is incorporated herein by reference in its entirety.

BACKGROUND

1. Field of the Invention

The invention relates to the technical field of the herbicides, in particular that of the herbicides for the selective control of broad-leaved weeds and weed grasses in crops of useful plants.

2. Description of Related Art

WO2003/010143 and WO2003/010153 disclose certain N-(tetrazol-5-yl)- and N-(triazol-5-yl)benzamides and their pharmacological action. The compound N-(1-propyltetrazol-5-yl)-2,4-dichlorobenzamide is known under the CAS-No. 639048-78-5. These publications do not disclose any herbicidal action of these compounds.

SUMMARY

It has now been found that N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides are particularly suitable as herbicides.

Accordingly, the present invention provides N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the formula (I) or salts thereof

in which

A represents N or CY,

B represents N or CH,

X represents nitro, halogen, cyano, formyl, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, C(O)NR¹OR¹, OR¹, OCOR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², NR₁R₂, P(O)(OR⁵)₂, CH₂P(O)(OR⁵)₂, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups,

Y represents hydrogen, nitro, halogen, cyano, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, CO(NOR¹)R¹, NR¹SO₂R², NR¹COR¹, OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂ (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO2R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-CN, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², N(R¹)₂, P(O)(OR⁵)₂, CH₂P(O)(OR⁵)₂, (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups,

Z represents halogen, cyano, thiocyanato, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, C(O)NR¹OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², N(R¹)₂, P(O)(OR⁵)₂, heteroaryl, heterocyclyl or phenyl, where the three last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₃-C₆)-cycloalkyl, S(O)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy and halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups, or

Z may also represent hydrogen, (C₁-C₆)-alkyl or (C₁-C₆)-alkoxy if Y represents the radical S(O)_(n)R²,

R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, CH₂R⁶, heteroaryl, heterocyclyl or phenyl, where the three last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl,

R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-haloalkenyl, (C₂-C₆)-alkynyl, (C₂-C₆)-haloalkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, (C₃-C₆)-halocycloalkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocycl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl, (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 21 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, thiocyanato, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR³, OCOR³, SCOR⁴, NR³COR³, NR³SO₂R⁴, CO₂R³, COSR⁴, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups,

R² represents (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-haloalkenyl, (C₂-C₆)-alkynyl, (C₂-C₆)-haloalkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, (C₃-C₆)-halocycloalkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl, (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 21 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, thiocyanato, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR³, OCOR³, SCOR⁴, NR³COR³, NR³SO₂R⁴, CO₂R³, COSR⁴, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups,

R3 represents hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C6)-cycloalkyl or (C3-C6)-cycloalkyl-(C1-C6)-alkyl,

R4 represents (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-alkynyl,

R5 represents methyl or ethyl,

R6 represents acetoxy, acetamido, N-methylacetamido, benzoyloxy, benzamido, N-methylbenzamido, methoxycarbonyl, ethoxycarbonyl, benzoyl, methylcarbonyl, piperidinylcarbonyl, morpholinylcarbonyl, trifluoromethylcarbonyl, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, (C₁-C₆)-alkoxy, (C₃-C₆)-cycloalkyl or represents heteroaryl, heterocyclyl or phenyl, each of which is substituted by s radicals from the group consisting of methyl, ethyl, methoxy, trifluoromethyl and halogen,

n represents 0, 1 or 2, s represents 0, 1, 2 or 3, with the proviso that X and Z both do not represent chlorine and B does not represent nitrogen if R represents n-propyl.

DETAILED DESCRIPTION OF A PREFERRED EMBODIMENT

In formula (I) and all the formulae below, alkyl radicals having more than two carbon atoms can be straight-chain or branched. Alkyl radicals are, for example, methyl, ethyl, n- or isopropyl, n-, iso-, t- or 2-butyl, pentyls, hexyls, such as n-hexyl, isohexyl and 1,3-dimethylbutyl. Halogen represents fluorine, chlorine, bromine or iodine.

Heterocyclyl is a saturated, partially saturated or fully unsaturated cyclic radical which contains 3 to 6 ring atoms, 1 to 4 of which are from the group consisting of oxygen, nitrogen and sulfur, and which may additionally be fused to a benzo ring. Heterocyclyl is, for example, piperidinyl, pyrrolidinyl, tetrahydrofuranyl, dihydrofuranyl and oxetanyl.

Heteroaryl is an aromatic cyclic radical which contains 3 to 6 ring atoms, 1 to 4 of which are from the group consisting of oxygen, nitrogen and sulfur, and which may additionally be fused to a benzo ring. Heteroaryl is, for example, benzimidazol-2-yl, furanyl, imidazolyl, isoxazolyl, isothiazolyl, oxazolyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyridinyl, benzisoxazolyl, thiazolyl, pyrrolyl, pyrazolyl, thiophenyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl, 1,2,4-triazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,3-thiadiazolyl, 1,2,5-thiadiazolyl, 2H-1,2,3,4-tetrazolyl, 1H-1,2,3,4-tetrazolyl, 1,2,3,4-oxatriazolyl, 1,2,3,5-oxatriazolyl, 1,2,3,4-thiatriazolyl and 1,2,3,5-thiatriazolyl.

Where a group is substituted by a plurality of radicals, this means that this group is substituted by one or more identical or different representatives of the radicals mentioned.

Depending on the nature and the attachment of the substituents, the compounds of the formula (I) may be present as stereoisomers. If, for example, one or more asymmetrically substituted carbon atoms are present, there may be enantiomers and diastereomers. There may also be stereoisomers if n is 1 (sulfoxides). Stereoisomers may be obtained from the mixtures resulting from the preparation using customary separation methods, for example by chromatographic separation techniques. It is also possible to prepare stereoisomers selectively by using stereoselective reactions employing optically active starting materials and/or auxiliaries. The invention also relates to all stereoisomers and mixtures thereof embraced by the formula (I) but not specifically defined.

Preference is given to compounds of the formula (I) in which

A represents N or CY,

B represents N or CH,

X represents nitro, halogen, cyano, thiocyanato, (C1-C6)-alkyl, halo-(C1-C6)-alkyl, (C2-C6)-alkenyl, halo-(C2-C6)-alkenyl, (C2-C6)-alkynyl, halo-(C3-C6)-alkynyl, (C3-C6)-cycloalkyl, halo-(C3-C6)-cycloalkyl, (C1-C6)-alkyl-O-(C1-C6)-alkyl, (C3-C6)-cycloalkyl-(C1-C6)-alkyl, halo-(C3-C6)-cycloalkyl-(C1-C6)-alkyl, COR1, OR1, OCOR1, OSO2R2, S(O)nR2, SO2OR1, SO2N(R1)2, NR1SO2R2, NR1COR1, (C1-C6)-alkyl-S(O)nR2, (C1-C6)-alkyl-OR1, (C1-C6)-alkyl-OCOR1, (C1-C6)-alkyl-OSO2R2, (C1-C6)-alkyl-CO2R1, (C1-C6)-alkyl-SO2OR1, (C1-C6)-alkyl-CON(R1)2, (C1-C6)-alkyl-SO2N(R1)2, (C1-C6)-alkyl-NR1COR1 or (C1-C6)-alkyl-NR1SO2R2, (C1-C6)-alkyl-heteroaryl, (C1-C6)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C1-C6)-alkyl, halo-(C1-C6)-alkyl, S(O)n-(C1-C6)-alkyl, (C1-C6)-alkoxy, halo-(C1-C6)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups,

Y represents hydrogen, nitro, halogen, cyano, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, OR¹, COOR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂ N(R¹)₂, N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups,

Z represents halogen, cyano, thiocyanato, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, C(O)N(R¹)₂, C(O)NR¹OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², 1,2,4-triazol-1-yl, or

Z may also represent hydrogen, (C₁-C₆)-alkyl or (C₁-C₆)-alkoxy if Y represents the radical S(O)_(n)R²,

R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₃-C₇)-cycloalkylmethyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, acetylmethyl, methoxymethyl, or represents phenyl or benzyl which are substituted by s radicals from the group consisting of methyl, methoxy, trifluoromethyl and halogen,

R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 16 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR^(S), OCOR³, NR³COR³, NR³SO₂R⁴, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups,

R² represents (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where these radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, NR³SO₂R⁴, COR³, OCOR³, NR³COR³, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups,

R³ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl or (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl,

R⁴ represents (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl,

n represents 0, 1 or 2, s represents 0, 1, 2 or 3.

Particular preference is given to compounds of the formula (I) in which

A represents N or CY,

B represents N or CH,

X represents nitro, halogen, cyano, (C1-C6)-alkyl, halo-(C1-C6)-alkyl, (C3-C6)-cycloalkyl, OR¹, S(O)_(n)R², (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups,

Y represents hydrogen, nitro, halogen, cyano, (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, OR¹, S(O)_(n)R², SO₂N(R¹)₂, N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups,

Z represents halogen, cyano, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)R², 1,2,4-triazol-1-yl, or Z may also represent hydrogen, methyl, methoxy or ethoxy if Y represents the radical S(O)_(n)R²,

R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₃-C₇)-cycloalkylmethyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, acetylmethyl or methoxymethyl, or represents phenyl which is substituted by s radicals from the group consisting of methyl, methoxy, trifluoromethyl and halogen;

R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 16 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR^(S), OCOR³, NR³COR³, NR³SO₂R⁴, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups,

R² represents (C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl or (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, where the three radicals mentioned above are each substituted by s radicals from the group consisting of halogen and OR³,

R³ represents hydrogen or (C₁-C₆)-alkyl,

R⁴ represents (C₁-C₆)-alkyl,

n represents 0, 1 or 2,

s represents 0, 1, 2 or 3.

In all formulae given below, the substituents and symbols have, unless defined otherwise, the same meaning as described under formula (I).

Compounds according to the invention can be prepared, for example, by the method given in Scheme 1 by base-catalyzed reaction of a benzoyl chloride (II) with a 5-amino-1-H-1,2,4-triazole or 5-amino-1H-tetrazole (III):

The benzoyl chlorides of the formula (II) or the benzoic acids on which they are based are known in principle and can be prepared, for example, according to the methods described in U.S. Pat. No. 6,376,429 B1, EP 1 585 742 A1 and EP 1 202 978 A1.

Compounds according to the invention can also be prepared by the method given in Scheme 2 by reacting a benzoic acid of the formula (IV) with a 5-amino-1-H-1,2,4-triazole or 5-amino-1H-tetrazole (III):

For the activation, use may be made of dehydrating agents usually employed for amidation reactions, for example 1,1′-carbonyldiimidazole (CDI), dicyclohexylcarbodiimide (DCC), 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane 2,4,6-trioxide (T3P) etc.

Compounds according to the invention can also be prepared by the method given in Scheme 3 by reacting an N-(1H-1,2,4-triazol-5-yl)benzamide, N-(1H-tetrazol-5-yl)benzamide, N-(1H-1,2,4-triazol-5-yl)nicotinamide or N-(1H-tetrazol-5-yl)nicotinamide:

For the reaction given in Scheme 3, it is possible to use, for example, alkylating agents such as alkyl halides, alkylsulfonates or dialkyl sulfates in the presence of a base.

It may be expedient to change the order of reaction steps. Thus, benzoic acids carrying a sulfoxide can not be converted directly into their acid chlorides. Here, it is advisable to prepare initially, at the thioether stage, the amide and then to oxidize the thioether to the sulfoxide.

The 5-amino-1H-tetrazoles of the formula (III) are either commercially available or can be prepared analogously to methods known from the literature. For example, 5-amino-1-R-tetrazoles can be prepared according to the method described in Journal of the American Chemical Society (1954), 76, 923-924 from aminotetrazole:

In the formula mentioned above, R represents, for example, an alkyl radical. 5-Amino-1-R-tetrazoles can be synthesized, for example, as described in Journal of the American Chemical Society (1954) 76, 88-89:

The 5-amino-1H-triazoles of the formula (III) are either commercially available or can be prepared analogously to methods known from the literature. For example, 5-amino-1-R-triazoles can be prepared according to the method described in Zeitschrift für Chemie (1990), 30(12), 436-437 from aminotriazole:

5-Amino-1-R-triazoles can also be synthesized as described, for example, in Chemische Berichte (1964), 97(2), 396-404:

5-Amino-1-R-triazoles can also be synthesized as described, for example, in Angewandte Chemie (1963), 75, 918:

Collections of compounds of the formula (I) and/or salts thereof which can be synthesized by the aforementioned reactions can also be prepared in a parallel manner, it being possible for this to take place in a manual, partly automated or completely automated manner. In this connection, it is, for example, possible to automate the reaction procedure, the work-up or the purification of the products and/or intermediates. Overall, this is understood as meaning a procedure as described, for example, by D. Tiebes in Combinatorial Chemistry—Synthesis, Analysis, Screening (editor Günther Jung), Verlag Wiley 1999, on pages 1 to 34.

For the parallel reaction procedure and work-up, it is possible to use a series of commercially available instruments, for example Calpyso reaction blocks from Barnstead International, Dubuque, Iowa 52004-0797, USA or reaction stations from Radleys, Shirehill, Saffron Walden, Essex, CB 11 3AZ, England or MuItiPROBE Automated Workstations from Perkin Elmer, Waltham, Mass. 02451, USA. For the parallel purification of compounds of the formula (I) and salts thereof or of intermediates produced during the preparation, there are available, inter alia, chromatography apparatuses, for example from ISCO, Inc., 4700 Superior Street, Lincoln, Nebr. 68504, USA.

The apparatuses listed lead to a modular procedure in which the individual process steps are automated, but between the process steps manual operations have to be carried out. This can be circumvented by using partly or completely integrated automation systems in which the respective automation modules are operated, for example, by robots. Automation systems of this type can be acquired, for example, from Caliper, Hopkinton, Mass. 01748, USA.

The implementation of single or several synthesis steps can be supported through the use of polymer-supported reagents/scavenger resins. The specialist literature describes a series of experimental protocols, for example in ChemFiles, Vol. 4, No. 1, Polymer-Supported Scavengers and Reagents for Solution-Phase Synthesis (Sigma-Aldrich).

Besides the methods described here, the preparation of compounds of the formula (I) and salts thereof can take place completely or partially by solid-phase supported methods. For this purpose, individual intermediates or all intermediates in the synthesis or a synthesis adapted for the corresponding procedure are bonded to a synthesis resin. Solid-phase supported synthesis methods are sufficiently described in the specialist literature, e.g. Barry A. Bunin in “The Combinatorial Index”, Verlag Academic Press, 1998 and Combinatorial Chemistry—Synthesis, Analysis, Screening (editor Gunther Jung), Verlag Wiley, 1999. The use of solid-phase supported synthesis methods permits a series of protocols known in the literature, which again can be carried out manually or in an automated manner. The reactions can be carried out, for example, by means of IRORI technology in microreactors from Nexus Biosystems, 12140 Community Road, Poway, Calif. 92064, USA.

Both on a solid phase and in liquid phase can the procedure of individual or several synthesis steps be supported through the use of microwave technology. The specialist literature describes a series of experimental protocols, for example in Microwaves in Organic and Medicinal Chemistry (editor C. O. Kappe and A. Stadler), Verlag Wiley, 2005.

The preparation according to the process described here produces compounds of the formula (I) and their salts in the form of substance collections which are called libraries. The present invention also provides libraries which comprise at least two compounds of the formula (I) and their salts.

The compounds of the formula (I) according to the invention (and/or their salts), hereinbelow also referred to together as “compounds according to the invention”, have excellent herbicidal efficacy against a broad spectrum of economically important monocotyledonous and dicotyledonous annual harmful plants. The active compounds act efficiently even on perennial weeds which produce shoots from rhizomes, root stocks and other perennial organs and which are difficult to control.

The present invention therefore also relates to a method of controlling unwanted plants or for regulating the growth of plants, preferably in crops of plants, where one or more compound(s) according to the invention is/are applied to the plants (for example harmful plants such as monocotyledonous or dicotyledonous weeds or undesired crop plants), to the seeds (for example grains, seeds or vegetative propagules such as tubers or shoot parts with buds) or to the area on which the plants grow (for example the area under cultivation). In this context, the compounds according to the invention can be applied for example pre-sowing (if appropriate also by incorporation into the soil), pre-emergence or post-emergence. Specific examples may be mentioned of some representatives of the monocotyledonous and dicotyledonous weed flora which can be controlled by the compounds according to the invention, without the enumeration being restricted to certain species.

Monocotyledonous harmful plants of the genera: Aegilops, Agropyron, Agrostis, Alopecurus, Apera, Avena, Brachiaria, Bromus, Cenchrus, Commelina, Cynodon, Cyperus, Dactyloctenium, Digitaria, Echinochloa, Eleocharis, Eleusine, Eragrostis, Eriochloa, Festuca, Fimbristylis, Heteranthera, Imperata, Ischaemum, Leptochloa, Lolium, Monochoria, Panicum, Paspalum, Phalaris, Phleum, Poa, Rottboellia, Sagittaria, Scirpus, Setaria, Sorghum.

Dicotyledonous weeds of the genera: Abutilon, Amaranthus, Ambrosia, Anoda, Anthemis, Aphanes, Artemisia, Atriplex, Bellis, Bidens, Capsella, Carduus, Cassia, Centaurea, Chenopodium, Cirsium, Convolvulus, Datura, Desmodium, Emex, Erysimum, Euphorbia, Galeopsis, Galinsoga, Galium, Hibiscus, Ipomoea, Kochia, Lamium, Lepidium, Lindernia, Matricaria, Mentha, Mercurialis, Mullugo, Myosotis, Papaver, Pharbitis, Plantago, Polygonum, Portulaca, Ranunculus, Raphanus, Rorippa, Rotala, Rumex, Salsola, Senecio, Sesbania, Sida, Sinapis, Solanum, Sonchus, Sphenoclea, Stellaria, Taraxacum, Thlaspi, Trifolium, Urtica, Veronica, Viola, Xanthium.

If the compounds according to the invention are applied to the soil surface before germination, the weed seedlings are either prevented completely from emerging or else the weeds grow until they have reached the cotyledon stage, but then their growth stops, and, eventually, after three to four weeks have elapsed, they die completely.

If the active compounds are applied post-emergence to the green parts of the plants, growth stops after the treatment, and the harmful plants remain at the growth stage of the point of time of application, or they die completely after a certain time, so that in this manner competition by the weeds, which is harmful to the crop plants, is eliminated very early and in a sustained manner.

Although the compounds according to the invention display an outstanding herbicidal activity against monocotyledonous and dicotyledonous weeds, crop plants of economically important crops, for example dicotyledonous crops of the genera Arachis, Beta, Brassica, Cucumis, Cucurbita, Helianthus, Daucus, Glycine, Gossypium, Ipomoea, Lactuca, Linum, Lycopersicon, Nicotiana, Phaseolus, Pisum, Solanum, Vicia, or monocotyledonous crops of the genera Allium, Ananas, Asparagus, Avena, Hordeum, Oryza, Panicum, Saccharum, Secale, Sorghum, Triticale, Triticum, Zea, in particular Zea and Triticum, are damaged only to an insignificant extent, or not at all, depending on the structure of the respective compound according to the invention and its application rate. This is why the present compounds are highly suitable for the selective control of unwanted plant growth in plant crops such as agriculturally useful plants or ornamentals.

Moreover, the compounds according to the invention (depending on their respective structure and the application rate applied) have outstanding growth-regulatory properties in crop plants. They engage in the plant metabolism in a regulatory fashion and can therefore be employed for the influencing, in a targeted manner, of plant constituents and for facilitating harvesting, such as, for example, by triggering desiccation and stunted growth. Moreover, they are also suitable for generally controlling and inhibiting unwanted vegetative growth without destroying the plants in the process. Inhibiting the vegetative growth plays an important role in many monocotyledonous and dicotyledonous crops since for example lodging can be reduced, or prevented completely, hereby.

By virtue of their herbicidal and plant-growth-regulatory properties, the active compounds can also be employed for controlling harmful plants in crops of genetically modified plants or plants modified by conventional mutagenesis. In general, the transgenic plants are distinguished by especially advantageous properties, for example by resistances to certain pesticides, mainly certain herbicides, resistances to plant diseases or causative organisms of plant diseases, such as certain insects or microorganisms such as fungi, bacteria or viruses. Other specific characteristics relate, for example, to the harvested material with regard to quantity, quality, storeability, composition and specific constituents. Thus, transgenic plants are known whose starch content is increased, or whose starch quality is altered, or those where the harvested material has a different fatty acid composition.

It is preferred, with respect to transgenic crops, to use the compounds according to the invention in economically important transgenic crops of useful plants and ornamentals, for example of cereals such as wheat, barley, rye, oats, millet, rice and corn or else crops of sugar beet, cotton, soybean, oilseed rape, potato, tomato, peas and other vegetables. It is preferred to employ the compounds according to the invention as herbicides in crops of useful plants which are resistant, or have been made resistant by recombinant means, to the phytotoxic effects of the herbicides.

It is preferred to use the compounds according to the invention or their salts in economically important transgenic crops of useful plants and ornamentals, for example of cereals such as wheat, barley, rye, oats, millet, rice, cassaya and corn or else crops of sugar beet, cotton, soybean, oilseed rape, potato, tomato, peas and other vegetables. It is preferred to employ the compounds according to the invention as herbicides in crops of useful plants which are resistant, or have been made resistant by recombinant means, to the phytotoxic effects of the herbicides.

Conventional methods of generating novel plants which have modified properties in comparison to plants occurring to date consist, for example, in traditional breeding methods and the generation of mutants. Alternatively, novel plants with altered properties can be generated with the aid of recombinant methods (see, for example, EP-A-0221044, EP-A-0131624). For example, the following have been described in several cases:

-   -   the modification, by recombinant technology, of crop plants with         the aim of modifying the starch synthesized in the plants (for         example WO 92/11376, WO 92/14827, WO 91/19806),     -   transgenic crop plants which are resistant to certain herbicides         of the glufosinate type (cf., for example, EP-A-0242236,         EP-A-242246) or of the glyphosate type (WO 92/00377) or of the         sulfonylurea type (EP-A-0257993, U.S. Pat. No. 5,013,659),     -   transgenic crop plants, for example cotton, with the capability         of producing Bacillus thuringiensis toxins (Bt toxins), which         make the plants resistant to certain pests (EP-A-0142924,         EP-A-0193259),     -   transgenic crop plants with a modified fatty acid composition         (WO 91/13972),     -   genetically modified crop plants with novel constituents or         secondary metabolites, for example novel phytoalexins, which         bring about an increased disease resistance (EPA 309862,         EPA0464461),     -   genetically modified plants with reduced photorespiration which         feature higher yields and higher stress tolerance (EPA 0305398),     -   transgenic crop plants which produce pharmaceutically or         diagnostically important proteins (“molecular pharming”),     -   transgenic crop plants which are distinguished by higher yields         or better quality,     -   transgenic crop plants which are distinguished by a combination,         for example of the abovementioned novel properties (“gene         stacking”).

A large number of molecular-biological techniques by means of which novel transgenic plants with modified properties can be generated are known in principle; see, for example, I. Potrykus and G. Spangenberg (eds.) Gene Transfer to Plants, Springer Lab Manual (1995), Springer Verlag Berlin, Heidelberg. or Christou, “Trends in Plant Science” 1 (1996) 423-431.

To carry out such recombinant manipulations, nucleic acid molecules which allow mutagenesis or sequence changes by recombination of DNA sequences can be introduced into plasmids. For example, base substitutions can be carried out, part-sequences can be removed, or natural or synthetic sequences may be added with the aid of standard methods. To link the DNA fragments with one another, it is possible to add adapters or linkers to the fragments; see, for example, Sambrook et al., 1989, Molecular Cloning, A Laboratory Manual, 2nd ed., Cold Spring Harbor Laboratory Press, Cold Spring Harbor, N.Y.; or Winnacker “Gene and Klone” Genes and Clones, VCH Weinheim 2nd ed., 1996.

For example, the generation of plant cells with a reduced activity of a gene product can be achieved by expressing at least one corresponding antisense RNA, a sense RNA for achieving a cosuppression effect or by expressing at least one suitably constructed ribozyme which specifically cleaves transcripts of the abovementioned gene product. To this end, it is possible to use DNA molecules which encompass the entire coding sequence of a gene product inclusive of any flanking sequences which may be present, and also DNA molecules which only encompass portions of the coding sequence, it being necessary for these portions to be long enough to have an antisense effect in the cells. The use of DNA sequences which have a high degree of homology to the coding sequences of a gene product, but are not completely identical to them, is also possible.

When expressing nucleic acid molecules in plants, the protein synthesized can be localized in any desired compartment of the plant cell. However, to achieve localization in a particular compartment, it is possible, for example, to link the coding region with DNA sequences which ensure localization in a particular compartment. Such sequences are known to those skilled in the art (see, for example, Braun et al., EMBO J. 11 (1992), 3219-3227; Wolter et al., Proc. Natl. Acad. Sci. USA 85 (1988), 846-850; Sonnewald et al., Plant J. 1 (1991), 95-106). The nucleic acid molecules can also be expressed in the organelles of the plant cells.

The transgenic plant cells can be regenerated by known techniques to give rise to entire plants. In principle, the transgenic plants can be plants of any desired plant species, i.e. not only monocotyledonous, but also dicotyledonous, plants.

Thus, transgenic plants can be obtained whose properties are altered by overexpression, suppression or inhibition of homologous (=natural) genes or gene sequences or the expression of heterologous (=foreign) genes or gene sequences.

It is preferred to employ the compounds according to the invention in transgenic crops which are resistant to growth regulators such as, for example, dicamba, or to herbicides which inhibit essential plant enzymes, for example acetolactate synthases (ALS), EPSP synthases, glutamine synthases (GS) or hydroxyphenylpyruvate dioxygenases (HPPD), or to herbicides from the group of the sulfonylureas, the glyphosates, glufosinates or benzoylisoxazoles and analogous active compounds.

When the active compounds according to the invention are used in transgenic crops, effects are frequently observed—in addition to the effects on harmful plants which can be observed in other crops—which are specific for the application in the transgenic crop in question, for example a modified or specifically widened spectrum of weeds which can be controlled, modified application rates which may be employed for application, preferably good combinability with the herbicides to which the transgenic crop is resistant, and an effect on growth and yield of the transgenic crop plants.

The invention therefore also relates to the use of the compounds according to the invention as herbicides for controlling harmful plants in transgenic crop plants.

The compounds according to the invention can be used in the form of wettable powders, emulsifiable concentrates, sprayable solutions, dusting products or granules in the customary formulations. The invention therefore also provides herbicidal and plant growth-regulating compositions which comprise the compounds according to the invention.

The compounds according to the invention can be formulated in various ways according to which biological and/or physicochemical parameters are required. Possible formulations include, for example: wettable powders (WP), water-soluble powders (SP), water-soluble concentrates, emulsifiable concentrates (EC), emulsions (EW) such as oil-in-water and water-in-oil emulsions, sprayable solutions, suspension concentrates (SC), oil- or water-based dispersions, oil-miscible solutions, capsule suspensions (CS), dusting products (DP), seed-dressing products, granules for scattering and soil application, granules (GR) in the form of microgranules, spray granules, coated granules and adsorption granules, water-dispersible granules (WG), water-soluble granules (SG), ULV formulations, microcapsules and waxes. These individual types of formulation are known in principle and are described, for example, in: Winnacker-Kuchler, “Chemische Technologie” [Chemical technology], Volume 7, C. Hanser Verlag Munich, 4th Ed. 1986, Wade van Valkenburg, “Pesticide Formulations”, Marcel Dekker, N.Y., 1973; K. Martens, “Spray Drying” Handbook, 3rd Ed. 1979, G. Goodwin Ltd. London.

The necessary formulation assistants, such as inert materials, surfactants, solvents and further additives, are likewise known and are described, for example, in: Watkins, “Handbook of Insecticide Dust Diluents and Carriers”, 2nd Ed., Darland Books, Caldwell N.J., H.v. Olphen, “Introduction to Clay Colloid Chemistry”; 2nd Ed., J. Wiley & Sons, N.Y.; C. Marsden, “Solvents Guide”; 2nd Ed., Interscience, N.Y. 1963; McCutcheon's “Detergents and Emulsifiers Annual”, MC Publ. Corp., Ridgewood N.J.; Sisley and Wood, “Encyclopedia of Surface Active Agents”, Chem. Publ. Co. Inc., N.Y. 1964; Schonfeldt, “Grenzflächenaktive Äthylenoxidaddukte” [Interface-active ethylene oxide adducts], Wiss. Verlagsgesell., Stuttgart 1976; Winnacker-Küchler, “Chemische Technologie”, Volume 7, C. Hanser Verlag Munich, 4th Ed. 1986.

Based on these formulations, it is also possible to produce combinations with other pesticidally active compounds, such as, for example, insecticides, acaricides, herbicides, fungicides, and also with safeners, fertilizers and/or growth regulators, for example in the form of a finished formulation or as a tank mix. Suitable safeners are, for example, mefenpyr-diethyl, cyprosulfamid, isoxadifen-ethyl, cloquintocet-mexyl and dichlormid.

Wettable powders are preparations which can be dispersed uniformly in water and, as well as the active compound, apart from a diluent or inert substance, also comprise surfactants of the ionic and/or nonionic type (wetting agents, dispersants), for example polyoxyethylated alkylphenols, polyoxyethylated fatty alcohols, polyoxyethylated fatty amines, fatty alcohol polyglycol ether sulfates, alkanesulfonates, alkylbenzenesulfonates, sodium lignosulfonate, sodium 2,2′-dinaphthylmethane-6,6′-disulfonate, sodium dibutylnaphthalenesulfonate or else sodium oleylmethyltauride. To prepare the wettable powders, the herbicidally active compounds are ground finely, for example in customary apparatus such as hammer mills, blower mills and air-jet mills and simultaneously or subsequently mixed with the formulation assistants.

Emulsifiable concentrates are prepared by dissolving the active compound in an organic solvent, for example butanol, cyclohexanone, dimethylformamide, xylene or else relatively high-boiling aromatics or hydrocarbons or mixtures of the organic solvents with addition of one or more surfactants of the ionic and/or nonionic type (emulsifiers). The emulsifiers used may, for example, be: calcium alkylarylsulfonate salts such as calcium dodecylbenzenesulfonate, or nonionic emulsifiers such as fatty acid polyglycol esters, alkylaryl polyglycol ethers, fatty alcohol polyglycol ethers, propylene oxide-ethylene oxide condensation products, alkyl polyethers, sorbitan esters, for example sorbitan fatty acid esters, or polyoxyethylene sorbitan esters, for example polyoxyethylene sorbitan fatty acid esters.

Dusts are obtained by grinding the active compound with finely distributed solid substances, for example talc, natural clays, such as kaolin, bentonite and pyrophyllite, or diatomaceous earth.

Suspension concentrates may be water- or oil-based. They may be prepared, for example, by wet grinding by means of commercial bead mills and optional addition of surfactants as have, for example, already been listed above for the other formulation types.

Emulsions, for example oil-in-water emulsions (EW), can be prepared, for example, by means of stirrers, colloid mills and/or static mixers using aqueous organic solvents and optionally surfactants, as have, for example, already been listed above for the other formulation types.

Granules can be prepared either by spraying the active compound onto granular inert material capable of adsorption or by applying active compound concentrates to the surface of carrier substances, such as sand, kaolinites or granular inert material, by means of adhesives, for example polyvinyl alcohol, sodium polyacrylate or mineral oils. Suitable active compounds can also be granulated in the manner customary for the preparation of fertilizer granules—if desired as a mixture with fertilizers.

Water-dispersible granules are prepared generally by the customary processes such as spray-drying, fluidized bed granulation, pan granulation, mixing with high-speed mixers and extrusion without solid inert material.

For the preparation of pan, fluidized bed, extruder and spray granules, see, for example, processes in “Spray-Drying Handbook” 3rd ed. 1979, G. Goodwin Ltd., London; J. E. Browning, “Agglomeration”, Chemical and Engineering 1967, pages 147 ff; “Perry's Chemical Engineer's Handbook”, 5th Ed., McGraw-Hill, New York 1973, p. 8-57.

For further details regarding the formulation of crop protection compositions, see, for example, G. C. Klingman, “Weed Control as a Science”, John Wiley and Sons, Inc., New York, 1961, pages 81-96 and J. D. Freyer, S. A. Evans, “Weed Control Handbook”, 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pages 101-103.

The agrochemical formulations contain generally from 0.1 to 99% by weight, in particular from 0.1 to 95% by weight, of compounds according to the invention. In wettable powders, the active compound concentration is, for example, from about 10 to 90% by weight, the remainder to 100% by weight consisting of customary formulation components. In the case of emulsifiable concentrates, the active compound concentration can be from about 1 to 90, preferably from 5 to 80, % by weight. Formulations in the form of dusts comprise from 1 to 30% by weight of active compound, preferably usually from 5 to 20% by weight of active compound; sprayable solutions contain from about 0.05 to 80% by weight, preferably from 2 to 50% by weight of active compound. In the case of water-dispersible granules, the active compound content depends partially on whether the active compound is present in liquid or solid form and on which granulation auxiliaries, fillers, etc., are used. In the water-dispersible granules, the content of active compound is, for example, between 1 and 95% by weight, preferably between 10 and 80% by weight.

In addition, the active compound formulations mentioned optionally comprise the respective customary adhesives, wetting agents, dispersants, emulsifiers, penetrants, preservatives, antifreeze agents and solvents, fillers, carriers and dyes, defoamers, evaporation inhibitors and agents which influence the pH and the viscosity.

Based on these formulations, it is also possible to produce combinations with other pesticidally active compounds, such as, for example, insecticides, acaricides, herbicides, fungicides, and also with safeners, fertilizers and/or growth regulators, for example in the form of a finished formulation or as a tank mix.

Active compounds which can be employed in combination with the compounds according to the invention in mixed formulations or in the tank mix are, for example, known active compounds which are based on the inhibition of, for example, acetolactate synthase, acetyl-CoA carboxylase, cellulose synthase, enolpyruvylshikimate-3-phosphate synthase, glutamine synthetase, p-hydroxyphenylpyruvate dioxygenase, phytoene desaturase, photosystem I, photosystem II, protoporphyrinogen oxidase, as are described in, for example, Weed Research 26 (1986) 441-445 or “The Pesticide Manual”, 15th edition, The British Crop Protection Council and the Royal Soc. of Chemistry, 2009 and the literature cited therein. Known herbicides or plant growth regulators which can be combined with the compounds according to the invention are, for example, the following active compounds (the compounds are either designated by the common name according to the International Organization for Standardization (ISO) or by the chemical name, or by the code number) and always comprise all use forms such as acids, salts, esters and isomers such as stereoisomers and optical isomers. Here, by way of example, one and in some cases a plurality of use forms are mentioned:

acetochlor, acibenzolar, acibenzolar-S-methyl, acifluorfen, acifluorfen-sodium, aclonifen, alachlor, allidochlor, alloxydim, alloxydim-sodium, ametryn, amicarbazone, amidochlor, amidosulfuron, aminocyclopyrachlor, aminopyralid, amitrole, ammonium sulfamate, ancymidol, anilofos, asulam, atrazine, azafenidin, azimsulfuron, aziprotryn, beflubutamid, benazolin, benazolin-ethyl, bencarbazone, benfluralin, benfuresate, bensulide, bensulfuron, bensulfuron-methyl, bentazone, benzfendizone, benzobicyclon, benzofenap, benzofluor, benzoylprop, bicyclopyrone, bifenox, bilanafos, bilanafos-sodium, bispyribac, bispyribac-sodium, bromacil, bromobutide, bromofenoxim, bromoxynil, bromuron, buminafos, busoxinone, butachlor, butafenacil, butamifos, butenachlor, butralin, butroxydim, butylate, cafenstrole, carbetamide, carfentrazone, carfentrazone-ethyl, chlomethoxyfen, chloramben, chlorazifop, chlorazifop-butyl, chlorbromuron, chlorbufam, chlorfenac, chlorfenac-sodium, chlorfenprop, chlorflurenol, chlorflurenol-methyl, chloridazon, chlorimuron, chlorimuron-ethyl, chlormequat chloride, chlornitrofen, chlorophthalim, chlorthal-dimethyl, chlorotoluron, chlorsulfuron, cinidon, cinidon-ethyl, cinmethylin, cinosulfuron, clethodim, clodinafop, clodinafop-propargyl, clofencet, clomazone, clomeprop, cloprop, clopyralid, cloransulam, cloransulam-methyl, cumyluron, cyanamide, cyanazine, cyclanilide, cycloate, cyclosulfamuron, cycloxydim, cycluron, cyhalofop, cyhalofop-butyl, cyperquat, cyprazine, cyprazole, 2,4-D, 2,4-DB, daimuron/dymron, dalapon, daminozide, dazomet, n-decanol, desmedipham, desmetryn, detosyl pyrazolate (DTP), diallate, dicamba, dichlobenil, dichlorprop, dichlorprop-P, diclofop, diclofop-methyl, diclofop-P-methyl, diclosulam, diethatyl, diethatyl-ethyl, difenoxuron, difenzoquat, diflufenican, diflufenzopyr, diflufenzopyr-sodium, dimefuron, dikegulac-sodium, dimefuron, dimepiperate, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, dimethipin, dimetrasulfuron, dinitramine, dinoseb, dinoterb, diphenamid, dipropetryn, diquat, diquat dibromide, dithiopyr, diuron, DNOC, eglinazine-ethyl, endothal, EPTC, esprocarb, ethalfluralin, ethametsulfuron, ethametsulfuron-methyl, ethephon, ethidimuron, ethiozin, ethofumesate, ethoxyfen, ethoxyfen-ethyl, ethoxysulfuron, etobenzanid, F-5331, i.e. N-[2-chloro-4-fluoro-5-[4-(3-fluoropropyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]phenyl]-ethanesulfonamide, F-7967, i.e., 3-[7-chloro-5-fluoro-2-(trifluoromethyl)-1H-benzimidazol-4-yl]-1-methyl-6-(trifluoromethyl)pyrimidine-2,4(1H, 3H)dione, fenoprop, fenoxaprop, fenoxaprop-P, fenoxaprop-ethyl, fenoxaprop-P-ethyl, fenoxasulfone, fentrazamide, fenuron, flamprop, flamprop-M-isopropyl, flamprop-M-methyl, flazasulfuron, florasulam, fluazifop, fluazifop-P, fluazifop-butyl, fluazifop-P-butyl, fluazolate, flucarbazone, flucarbazone-sodium, flucetosulfuron, fluchloralin, flufenacet (thiafluamide), flufenpyr, flufenpyr-ethyl, flumetralin, flumetsulam, flumiclorac, flumiclorac-pentyl, flumioxazin, flumipropyn, fluometuron, fluorodifen, fluoroglycofen, fluoroglycofen-ethyl, flupoxam, flupropacil, flupropanate, flupyrsulfuron, flupyrsulfuron-methyl-sodium, flurenol, flurenol-butyl, fluridone, fluorochloridone, fluoroxypyr, fluoroxypyr-meptyl, flurprimidol, flurtamone, fluthiacet, fluthiacet-methyl, fluthiamide, fomesafen, foramsulfuron, forchlorfenuron, fosamine, furyloxyfen, gibberellic acid, glufosinate, glufosinate-ammonium, glufosinate-P, glufosinate-P-ammonium, glufosinate-P-sodium, glyphosate, glyphosate-isopropylammonium, H-9201, i.e., O-(2,4-dimethyl-6-nitrophenyl)-O-ethyl-isopropylphosphoramidothioate, halosafen, halosulfuron, halosulfuron-methyl, haloxyfop, haloxyfop-P, haloxyfop-ethoxyethyl, haloxyfop-P-ethoxyethyl, haloxyfop-methyl, haloxyfop-P-methyl, hexazinone, HW-02, i.e., 1-(dimethoxyphosphoryl)-ethyl(2,4-dichlorophenoxy)acetate, imazamethabenz, imazamethabenz-methyl, imazamox, imazamox-ammonium, imazapic, imazapyr, imazapyr-isopropylammonium, imazaquin, imazaquin-ammonium, imazethapyr, imazethapyr-ammonium,imazosulfuron, inabenfide, indanofan, indaziflam, indoleacetic acid (IAA), 4-indol-3-ylbutyric acid (IBA), iodosulfuron, iodosulfuron-methyl-sodium, ioxynil, ipfencarbazone, isocarbamid, isopropalin, isoproturon, isouron, isoxaben, isoxachlortole, isoxaflutole, isoxapyrifop, KUH-043, i.e., 3-({[5-(difluoromethyl)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}sulfonyl)-5,5-dimethyl-4,5-dihydro-1,2-oxazole, karbutilate, ketospiradox, lactofen, lenacil, linuron, maleic hydrazide, MCPA, MCPB, MCPB-methyl, -ethyl and -sodium, mecoprop, mecoprop-sodium, mecoprop-butotyl, mecoprop-P-butotyl, mecoprop-P-dimethylammonium, mecoprop-P-2-ethylhexyl, mecoprop-P-potassium, mefenacet, mefluidide, mepiquat-chloride, mesosulfuron, mesosulfuron-methyl, mesotrione, methabenzthiazuron, metam, metamifop, metamitron, metazachlor, metazasulfuron, methazole, methiopyrsulfuron, methiozolin, methoxyphenone, methyldymron, 1-methylcyclopropene, methylisothiocyanate, metobenzuron, metobromuron, metolachlor, S-metolachlor, metosulam, metoxuron, metribuzin, metsulfuron, metsulfuron-methyl, molinate, monalide, monocarbamide, monocarbamide dihydrogensulfate, monolinuron, monosulfuron, monosulfuron-ester, monuron, MT 128, i.e., 6-chloro-N-[(2E)-3-chloroprop-2-en-1-yl]-5-methyl-N-phenylpyridazin-3-amine, MT-5950, i.e. N-[3-chloro-4-(1-methylethyl)phenyl]-2-methylpentanamide, NGGC-011, naproanilide, napropamide, naptalam, NC-310, i.e. 4-(2,4-dichlorobenzoyl)-1-methyl-5-benzyloxypyrazole, neburon, nicosulfuron, nipyraclofen, nitralin, nitrofen, nitrophenolate sodium (isomer mixture), nitrofluorfen, nonanoic acid, norflurazon, orbencarb, orthosulfamuron, oryzalin, oxadiargyl, oxadiazon, oxasulfuron, oxaziclomefone, oxyfluorfen, paclobutrazol, paraquat, paraquat-dichloride, pelargonic acid (nonanoic acid), pendimethalin, pendralin, penoxsulam, pentanochlor, pentoxazone, perfluidone, pethoxamid, phenisopham, phenmedipham, phenmedipham-ethyl, picloram, picolinafen, pinoxaden, piperophos, pirifenop, pirifenop-butyl, pretilachlor, primisulfuron, primisulfuron-methyl, probenazole, profluazol, procyazine, prodiamine, prifluraline, profoxydim, prohexadione, prohexadione-calcium, prohydrojasmone, prometon, prometryn, propachlor, propanil, propaquizafop, propazine, propham, propisochlor, propoxycarbazone, propoxycarbazone-sodium, propyrisulfuron, propyzamide, prosulfalin, prosulfocarb, prosulfuron, prynachlor, pyraclonil, pyraflufen, pyraflufen-ethyl, pyrasulfotole, pyrazolynate (pyrazolate), pyrazosulfuron, pyrazosulfuron-ethyl, pyrazoxyfen, pyribambenz, pyribambenz-isopropyl, pyribambenz-propyl, pyribenzoxim, pyributicarb, pyridafol, pyridate, pyriftalid, pyriminobac, pyriminobac-methyl, pyrimisulfan, pyrithiobac, pyrithiobac-sodium, pyroxasulfone, pyroxsulam, quinclorac, quinmerac, quinoclamine, quizalofop, quizalofop-ethyl, quizalofop-P, quizalofop-P-ethyl, quizalofop-P-tefuryl, rimsulfuron, saflufenacil, secbumeton, sethoxydim, siduron, simazine, simetryn, SN-106279, i.e. methyl-(2R)-2({7-[2-chloro-4-(trifluoromethyl)phenoxy]-2-naphthyl}oxy)propanoate, sulcotrione, sulfallate (CDEC), sulfentrazone, sulfometuron, sulfometuron-methyl, sulfosate (glyphosate-trimesium), sulfosulfuron, SYN-523, SYP-249, i.e., 1-ethoxy-3-methyl-1-oxobut-3-en-2-yl-5-[2-chloro-4-(trifluoromethyl)phenoxy]-2-nitrobenzoate, SYP-300, i.e., 1-[7-fluoro-3-oxo-4-(prop-2-yn-1-yl)-3,4-dihydro-2H-1,4-benzoxazin-6-yl]-3-propyl-2-thioxoimidazolidine-4,5-dione, tebutam, tebuthiuron, tecnazene, tefuryltrione, tembotrione, tepraloxydim, terbacil, terbucarb, terbuchlor, terbumeton, terbuthylazine, terbutryn, thenylchlor, thiafluamide, thiazafluoron, thiazopyr, thidiazimin, thidiazuron, thiencarbazone, thiencarbazone-methyl, thifensulfuron, thifensulfuron-methyl, thiobencarb, tiocarbazil, topramezone, tralkoxydim, triallate, triasulfuron, triaziflam, triazofenamide, tribenuron, tribenuron-methyl, trichloroacetic acid (TCA), triclopyr, tridiphane, trietazine, trifloxysulfuron, trifloxysulfuron-sodium, trifluralin, triflusulfuron, triflusulfuron-methyl, trimeturon, trinexapac, trinexapac-ethyl, tritosulfuron, tsitodef, uniconazole, uniconazole-P, vernolate, ZJ-0862 i.e. 3,4-dichloro-N-{2-[(4,6-dimethoxypyrimidin-2-yl)oxy]benzyl}aniline, and also the following compounds:

For application, the formulations present in commercial form are, if appropriate, diluted in a customary manner, for example in the case of wettable powders, emulsifiable concentrates, dispersions and water-dispersible granules with water. Preparations in the form of dusts, granules for soil application or granules for broadcasting and sprayable solutions are usually not diluted with other inert substances prior to application.

The required application rate of the compounds of the formula (I) varies according to the external conditions such as, inter alia, temperature, humidity and the type of herbicide used. It may vary within wide limits, for example between 0.001 and 1.0 kg/ha or more of active substance; however, preferably it is between 0.005 and 750 g/ha.

The examples below illustrate the invention:

Chemical Examples 1. Synthesis of 2-chloro-4-(methylsulfonyl)-N-(1-methyl-1,2,4-triazol-5-yl)-3-[(2,2,2-trifluoroethoxy)methyl])benzamide Table Example No. 1-258

At 90° C., 365 mg (1.0 mmol) of 2-chloro-4-(methylsulfonyl)-3-[(2,2,2-trifluoroethoxy)methyl])benzoyl chloride, 294 mg (1.0 mmol) of 1-methyl-1,2,4-triazol-5ylammonium sulfate and 12 mg (0.1 mmol) of DMAP in 3 ml of pyridine are stirred for 3 h. Most of the pyridine is then removed under reduced pressure, and ethyl acetate (EA) and 2N HCl are added to the residue. The organic phase is dried over Na₂SO₄, concentrated by evaporation and purified by RP-HPLC (acetonitrile/water). Yield 92 mg (21%).

2. Synthesis of 2-methyl-3-(methylsulfonyl)-N-(1-methyl-1,2,4-triazol-5-yl)-benzamide Table Example No. 1-90

At room temperature (RT), 297 mg (2.5 mmol) of thionyl chloride are added to 214 mg (1.0 mmol) of 2-methyl-3-(methylsulfonyl)benzoic acid, 220 mg (0.75 mmol) of 1-methyl-1,2,4-triazol-5ylammonium sulfate and 12 mg (0.1 mmol) of DMAP in 2 ml of pyridine. The mixture is stirred at 50° C. for 2 h. 0.1 ml of water is then added, and the mixture is stirred at RT for 30 min and 2N HCl is added. The product is filtered off with suction and dried. Yield 116 mg (39%).

3. Synthesis of 2,4-dichloro-N-(1-methyltetrazol-5-yl)benzamide Table Example No. 4-7

In a microwave oven, 209 mg (1.0 mmol) of 2,4-dichlorobenzoyl chloride, 198 mg (2.0 mmol) of 1-methyl-5-aminotetrazole and 237 mg (3 mmol) of pyridine in 3 ml of acetonitrile are stirred at 130° C. for 45 min. Water is then added, and the product is filtered off with suction and washed with ether. Yield 80 mg (30%).

4. Synthesis of 3-(pyrazol-1-yl)-2-methyl-4-(methylsulfonyl)-N-(1-methyltetrazol-5-yl)benzamide Table Example No. 4-152

At RT, 178 mg (1.5 mmol) of thionyl chloride are added to 280 mg (1.0 mmol) of 3-(pyrazol-1-yl)-2-methyl-4-(methylsulfonyl)benzoic acid, 148 mg (1.5 mmol) of 1-methyl-5-aminotetrazole and 12 mg (0.1 mmol) of DMAP in 2 ml of pyridine. The mixture is stirred at RT for 12 h and, after having been checked by LCMS, stirred at 50° C. for 3 h. 0.1 ml of water is then added, the mixture is stirred at RT for 30 min and 2N HCl is added. The product is filtered off with suction and dried. Yield 134 mg (37%).

5. Synthesis of 2-methyl-N-(1-methyltetrazol-5-yl)-6-trifluoromethylnicotinamide Table Example No. 8-19

At RT, 178 mg (1.5 mmol) of thionyl chloride are added to 205 mg (1.0 mmol) of 2-methyl-(6-trifluoromethyl)nicotinic acid, 148 mg (1.5 mmol) of 1-methyl-5-aminotetrazole and 12 mg (0.1 mmol) of DMAP in 2 ml of pyridine. The mixture is stirred at RT for 12 h and, after having been checked by LCMS, stirred at 50° C. for 2 h. 0.1 ml of water is then added, the mixture is stirred at RT for 30 min and EA and 2N HCl are added. The separated organic phase is washed once more with 2N HCl and sat. NaHCO₃ solution, dried over Na₂SO₄ and concentrated by evaporation. Yield 243 mg (85%).

The examples listed in the tables below were prepared analogously to methods identified above or can be obtained analogously to methods identified above. The compounds listed in the tables below are very particularly preferred.

The abbreviations used have the following meanings:

Et = ethyl Me = methyl n-Pr = n-propyl i-Pr = isopropyl c-Pr = cyclopropyl Ph = phenyl Ac = acetyl Bz = benzoyl

TABLE 1 Compounds of the formula (I) according to the invention in which A represents CY, B represents CH and R represents methyl

Physical data (¹H-NMR, DMSO-d₆, 400 No. X Y Z MHz) 1-1 F H Cl 1-2 F H Br 1-3 F H SO₂Me 1-4 F H SO₂Et 1-5 F H CF₃ 1-6 F H NO₂ 1-7 Cl H F 1-8 Cl H Cl 1-9 Cl H Br 11.23 (brs, 1H), 7.91 (s, 1H), 7.89 (s, 1H), 7.71 (d, 1H), 7.64 (d, 1H), 3.76 (s, 3H), 3.11 (s, 3H) 1-10 Cl H SMe 7.88 (s, 1H), 7.59 (d, 1H), 7.42 (d, 1H), 7.33 (dd, 1H), 3.74 (s, 3H), 2.55 (s, 3H) 1-11 Cl H SOMe 1-12 Cl H SO₂Me 8.07 (s, 1H), 7.94 (dd, 1H), 7.89 (d, 1H), 7.87 (s, 1H), 3.95 (s, 3H), 3.11 (s, 3H) 1-13 Cl H SO₂CH₂Cl 1-14 Cl H SEt 7.88 (s, 1H), 7.60 (d, 1H), 7.47 (d, 1H), 7.36 (dd, 1H), 3.74 (s, 3H), 3.10 (q, 2H), 1.27 (t, 3H) 1-15 Cl H SO₂Et 1-16 Cl H CF₃ 11.36 (brs, 1H), 8.06 (s, 1H), 7.95-7.88 (m, 3H), 3.79 (s, 3H), 3.11 (s, 3H) 1-17 Cl H NO₂ 1-18 Cl H pyrazol-1-yl 8.69 (d, 1H), 8.10 (d, 1H), 7.98 (dd, 1H), 7.89 (s, 1H), 7.84 (d, 1H), 7.83 (d, 1H), 6.62 (dd, 1H), 3.78 (s, 3H) 1-19 Cl H 1H-1,2,4-triazol-1- yl 1-20 Br H Cl 1-21 Br H Br 1-22 Br H SO₂Me 1-23 Br H SO₂Et 1-24 Br H CF₃ 8.17 (m, 1H), 7.90 (m, 3H), 3.80 (s, 3H), 3.29 (s, 3H), 2.73 (s, 3H) 1-25 SO₂Me H Cl 8.13 (d, 1H), 7.76 (d, 1H), 7.69 (dd, 1H), 7.59 (s, 1H), 3.92 (s, 3H), 3.39 (s, 3H) 1-26 SO₂Me H Br 8.14 (s, 1H), 8.12 (d, 1H), 7.92 (s, 1H), 7.80 (d, 1H), 3.79 (s, 3H), 3.43 (s, 3H) 1-27 SO₂Me H SMe 1-28 SO₂Me H SOMe 1-29 SO₂Me H SO₂Me 1-30 SO₂Me H SO₂Et 1-31 SO₂Me H CF₃ 8.38 (s, 1H), 7.95 (m, 2H), 7.54 (s, 1H), 3.89 (s, 3H), 3.40 (s, 3H) 1-32 SO₂Et H Cl 1-33 SO₂Et H Br 1-34 SO₂Et H SMe 1-35 SO₂Et H SOMe 1-36 SO₂Et H SO₂Me 1-37 SO₂Et H CF₃ 1-38 NO₂ H F 1-39 NO₂ H Cl 1-40 NO₂ H Br 1-41 NO₂ H I 1-42 NO₂ H CN 1-43 NO₂ H SO₂Me 8.29 (s, 1H), 8.16 (s, 2H), 7.84 (s, 1H), 3.77 (s, 3H), 3.12 (s, 3H) 1-44 NO₂ H SO₂Et 1-45 NO₂ H CF₃ 8.04-8.02 (m, 2H), 7.87 (d, 1H), 7.74 (s, 1H), 3.80 (s, 3H) 1-46 Me H Cl 7.88 (s, 1H), 7.62 (d, 1H), 7.45 (dd, 1H), 7.40 (dd, 1H), 3.73 (s, 3H), 2.43 (s, 3H) 1-47 Me H Br 1-48 Me H SMe 1-49 Me H SO₂Me 11.2 (brs, 1H), 7.92 (s, 2H), 7.87 (d, 1H), 7.83 (d, 1H), 3.77 (s, 3H), 3.27 (s, 3H), 2.52 (s, 3H) 1-50 Me H SO₂CH₂Cl 1-51 Me H SEt 1-52 Me H SO₂Et 1-53 Me H CF₃ 1-54 CH₂SO₂Me H CF₃ 1-55 Et H Cl 1-56 Et H Br 1-57 Et H SMe 1-58 Et H SO₂Me 1-59 Et H SO₂CH₂Cl 1-60 Et H SEt 1-61 Et H SO₂Et 1-62 Et H CF₃ 1-63 CF₃ H Cl 11.35 (brs, 1H), 7.99 (s, 1H), 7.95-7.85 (m, 3H), 3.74 (s, 3H) 1-64 CF₃ H Br 11.6 (brs, 1H), 7.85 (s, 1H), 7.71 (d, 1H), 7.48 (d, 1H), 7.24 (s, 1H), 3.79 (s, 3H) 1-65 CF₃ H SO₂Me 1-66 CF₃ H SO₂Et 1-67 CF₃ H CF₃ 8.22 (brs, 2H), 8.10 (brs, 1H), 7.93 (s, 1H), 3.76 (s, 3H) 1-68 NO₂ NH₂ F 1-69 NO₂ NHMe F 1-70 NO₂ NMe₂ F 1-71 NO₂ Me Cl 2.3 (s, 3H), 3.75 (s, 3H), 7.42 (d, 1H), 7.58 (s, 1H), 7.8 (d, 1H) 1-72 NO₂ NH₂ Cl 3.85 (s, 3H), 6.18 (s, 2H), 6.89 (s, 1H), 7.5 (s, 2H) 1-73 NO₂ NHMe Cl 1-74 NO₂ NMe₂ Cl 1-75 NO₂ NH₂ Br 1-76 NO₂ NHMe Br 1-77 NO₂ NMe₂ Br 1-78 NO₂ NH₂ CF₃ 3.85 (s, 3H), 6.05 (s, 2H), 6.98 (s, 1H), 7.55 (d, 1H), 7.68 (d, 1H) 1-79 NO₂ NMe₂ CF₃ 1-80 NO₂ NH₂ SO₂Me 1-81 NO₂ NH₂ SO₂Et 1-82 NO₂ NHMe SO₂Me 1-83 NO₂ NMe₂ SO₂Me 1-84 NO₂ NMe₂ SO₂Et 1-85 NO₂ NH₂ 1H-1,2,4-triazol-1- yl 1-86 NO₂ NHMe 1H-1,2,4-triazol-1- yl 1-87 NO₂ NMe₂ 1H-1,2,4-triazol-1- yl 1-88 Me SMe H 1-89 Me SOMe H 1-90 Me SO₂Me H 8.08 (d, 1H), 7.89 (s, 1H), 7.88 (d, 1H), 7.61 (t, 1H), 3.78 (s, 3H), 3.29 (s, 3H), 2.73 (s, 3H) 1-91 Me SEt H 1-92 Me SOEt H 1-93 Me SO₂Et H 1-94 Me S(CH₂)₂OMe H 1-95 Me SO(CH₂)₂OMe H 1-96 Me SO₂(CH₂)₂OMe H 1-97 Me F F 1-98 Me F Cl 1-99 Me SEt F 1-100 Me SOEt F 1-101 Me SO₂Et F 1-102 Me Me Cl 1-103 Me F Cl 1-104 Me Cl Cl 1-105 Me NH₂ Cl 1-106 Me NHMe Cl 1-107 Me NMe₂ Cl 1-108 Me O(CH₂)₂OMe Cl 7.88 (s, 1H), 7.46 (d, 1H), 7.37 (d, 1H), 4.05 (t, 2H), 3.74 (s, 3H), 3.68 (t, 2H), 3.30 (s, 3H), 2.37 (s, 3H) 1-109 Me O(CH₂)₃OMe Cl 1-110 Me O(CH₂)₄OMe Cl 1-111 Me OCH₂CONMe₂ Cl 1-112 Me O(CH₂)₂—CO—NMe₂ Cl 1-113 Me O(CH₂)₂—NH(CO)NMe₂ Cl 1-114 Me O(CH₂)₂—NH(CO)NHCO₂Et Cl 1-115 Me O(CH₂)₂—NHCO₂Me Cl 1-116 Me OCH₂—NHSO₂cPr Cl 1-117 Me O(CH₂)-5-2,4- Cl dimethyl-2,4- dihydro-3H-1,2,4- triazol-3-one 1-118 Me O(CH₂)-3,5- Cl dimethyl-1,2- oxazol-4-yl 1-119 Me SMe Cl 7.58 (s, 1H), 7.47 (d, 1H), 7.43 (d, 1H), 3.88 (s, 3H), 2.76 (s, 3H), 2.37 (s, 3H) 1-120 Me SOMe Cl 7.84 (s, 1H), 7.59 (d, 1H), 7.38 (d, 1H), 3.94 (s, 3H), 2.99 (s, 3H), 2.80 (s, 3H) 1-121 Me SO₂Me Cl 7.77 (s, 1H), 7.63 (d, 1H), 7.53 (d, 1H), 3.93 (s, 3H), 3.32 (s, 3H), 2.85 (s, 3H) 1-122 Me SEt Cl 7.88 (brs, 1H), 7.56 (brs, 2H), 3.75 (s, 3H), 2.85 (q, 2H), 2.64 (s, 3H), 1.13 (t, 3H) 1-123 Me SOEt Cl 7.61 (s, 1H), 7.58 (d, 1H), 7.35 (d, 1H), 3.88 (s, 3H), 3.30 (m, 1H), 3.09 (m, 1H), 2.75 (s, 3H), 1.36 (t, 3H) 1-124 Me SO₂Et Cl 7.61 (d, 1H), 7.51 (d, 1H), 7.50 (s, 1H), 3.88 (s, 3H), 3.45 (q, 2H), 2.83 (s, 3H), 1.35 (t, 3H) 1-125 Me S(CH₂)₂OMe Cl 1-126 Me SO(CH₂)₂OMe Cl 1-127 Me SO₂(CH₂)₂OMe Cl 1-128 Me NH₂ Br 1-129 Me NHMe Br 1-130 Me NMe₂ Br 1-131 Me OCH₂(CO)NMe₂ Br 1-132 Me O(CH₂)-5- Br pyrrolidin-2-one 1-133 Me SMe Br 1-134 Me SOMe Br 1-135 Me SO₂Me Br 1-136 Me SEt Br 1-137 Me SOEt Br 1-138 Me SO₂Et Br 1-139 Me SMe I 1-140 Me SOMe I 1-141 Me SO₂Me I 1-142 Me SEt I 1-143 Me SOEt I 1-144 Me SO₂Et I 1-145 Me Cl CF₃ 1-146 Me SMe CF₃ 1-147 Me SOMe CF₃ 1-148 Me SO₂Me CF₃ 7.88-7.80 (m, 3H), 3.86 (s, 3H), 3.37 (s, 3H), 2.88 (s, 3H) 1-149 Me SEt CF₃ 7.69 (d, 1H), 7.62 (d, 1H), 7.33 (s, 1H), 3.89 (s, 3H), 2.77 (s, 3H), 2.75 (q, 2H), 1.22 (t, 3H) 1-150 Me SOEt CF₃ 7.71 (d, 1H), 7.66 (d, 1H), 7.54 (s, 1H), 3.89 (s, 3H), 3.40 (m, 1H), 2.92-2.83 (m, 1H), 2.90 (s, 3H), 1.39 (t, 3H) 1-151 Me SO₂Et CF₃ 8.05 (brs, 2H), 7.92 (brs, 1H), 3.79 (s, 3H), 3.51 (q, 2H), 2.76 (s, 3H), 1.29 (t, 3H) 1-152 Me S(CH₂)₂OMe CF₃ 1-153 Me SO(CH₂)₂OMe CF₃ 1-154 Me SO₂(CH₂)₂OMe CF₃ 1-155 Me Me SO₂Me 1-156 Me 4,5-dihydro-1,2- SO₂Me oxazol-3-yl 1-157 Me 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 1-158 Me 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol- 3-yl 1-159 Me 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol- 3-yl 1-160 Me NH₂ SO₂Me 1-161 Me NHMe SO₂Me 2.42 (s, 3H), 2.98 (s, 3H), 3.08 (s, 3H), 3.88 (s, 3H), 5.62 (s, br, 1H), 7.22 (d, 1H), 7.42 (s, 1H), 7.8 (d, 1H) 1-162 Me NMe₂ SO₂Me 1-163 Me NH(CH₂)₂OMe SO₂Me 2.35 (s, 3H), 3.12 (s, 3H), 3.3 (m, 2H), 3.38 (s, 3H), 3.55 (m, 2H), 3.88 (s, 3H), 5.72 (s, 1H), 7.08 (d, 1H), 7.72 (d, 1H), 7.82 (s, 1H) 1-164 Me pyrazol-1-yl SO₂Me 8.14 (d, 1H), 7.98 (d, 1H), 7.81 (d, 1H), 7.73 (s, 1H), 7.71 (d, 1H), 6.56 (dd, 1H), 3.86 (s, 3H), 2.87 (s, 3H), 2.07 (s, 3H) 1-165 Me OH SO₂Me 1-166 Me OMe SO₂Me 1-167 Me OMe SO₂Et 1-168 Me OEt SO₂Me 1-169 Me OEt SO₂Et 1-170 Me OiPr SO₂Me 1-171 Me OiPr SO₂Et 1-172 Me O(CH₂)₂OMe SO₂Me 7.94 (d, 1H), 7.70 (s, 1H), 7.57 (d, 1H), 4.24 (t, 2H), 3.88 (s, 3H), 3.82 (t, 2H), 3.49 (s, 3H), 3.30 (s, 3H), 2.53 (s, 3H) 1-173 Me O(CH₂)₂OMe SO₂Et 1-174 Me O(CH₂)₃OMe SO₂Me 11.00 (s, 1H), 7.88 (s, 1H), 7.47 (d, 1H), 7.37 (d, 1H), 3.94 (t, 2H), 3.74 (s, 3H), 3.56 (t, 2H), 3.27 (s, 3H), 2.36 (s, 3H), 2.01 (quin, 2H) 1-175 Me O(CH₂)₃OMe SO₂Et 1-176 Me O(CH₂)₄OMe SO₂Me 1-177 Me O(CH₂)₄OMe SO₂Et 1-178 Me O(CH₂)₂NHSO2Me SO₂Me 1-179 Me O(CH₂)₂NHSO2Me SO₂Et 1-180 Me OCH₂(CO)NMe₂ SO₂Me 1-181 Me OCH₂(CO)NMe₂ SO₂Et 1-182 Me [1,4]dioxan-2- SO₂Me ylmethoxy 1-183 Me [1,4]dioxan-2- SO₂Et ylmethoxy 1-184 Me O(CH₂)₂—O(3,5-di- SO₂Me methoxypyrimidin- 2-yl) 1-185 Me Cl SO₂Me 1-186 Me SMe SO₂Me 1-187 Me SOMe SO₂Me 1-188 Me SO₂Me SO₂Me 8.28 (d, 1H), 7.88 (d, 1H), 7.74 (s, 1H), 3.85 (s, 3H), 3.56 (s, 3H), 3.46 (s, 3H), 2.83 (s, 3H) 1-189 Me SO₂Me SO₂Et 1-190 Me SEt SO₂Me 8.16 (d, 1H), 7.71 (d, 1H), 7.46 (s, 1H), 3.89 (s, 3H), 3.47 (s, 3H), 2.91 (q, 2H), 2.77 (s, 3H), 1.28 (t, 3H) 1-191 Me SOEt SO₂Me 8.05 (d, 1H), 7.78 (d, 1H), 7.66 (s, 1H), 3.87 (s, 3H), 3.47 (m, 1H), 3.35 (s, 3H), 3.24 (m, 1H), 2.91 (s, 3H), 1.52 (t, 3H) 1-192 Me SO₂Et SO₂Me 8.32 (d, 1H), 7.88 (d, 1H), 7.79 (s, 1H), 3.83 (s, 3H), 3.66 (q, 2H), 3.55 (s, 3H), 2.85 (s, 3H), 1.53 (t, 3H) 1-193 Me S(CH₂)₂OMe SO₂Me 1-194 Me SO(CH₂)₂OMe SO₂Me 1-195 Me SO₂(CH₂)₂OMe SO2Me 1-196 CH₂SMe OMe SO₂Me 1-197 CH₂OMe OMe SO₂Me 1-198 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 1-199 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 1-200 CH₂O(CH₂)₃OMe OMe SO₂Me 1-201 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 1-202 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 1-203 Et SMe Cl 1.20 (t, 3H), 2.40 (s, 3H), 3.12 (q, 2H), 3.88 (s, 3H), 7.12 (s, 1H), 7.45 (s, 2H) 1-204 Et SO₂Me Cl 1-205 Et SMe CF₃ 1.22 (t, 3H), 2.35 (s, 3H), 3.21 (q, 2H), 3.9 (s, 3H), 7.08 (s, 1H), 7.62 (d, 1H), 7.72 (d, 1H) 1-206 Et SO₂Me CF₃ 1-207 Et F SO₂Me 1-208 Et NH(CH₂)₂OMe SO₂Me 1-209 iPr SO₂Me CF₃ 1-210 cPr SO₂Me CF₃ 1-211 CF₃ O(CH₂)₂OMe F 1-212 CF₃ O(CH₂)₃OMe F 1-213 CF₃ OCH₂CONMe₂ F 1-214 CF₃ [1,4]dioxan-2- F ylmethoxy 1-215 CF₃ O(CH₂)₂OMe Cl 1-216 CF₃ O(CH₂)₃OMe Cl 1-217 CF₃ OCH₂CONMe₂ Cl 1-218 CF₃ [1,4]dioxan-2- Cl ylmethoxy 1-219 CF₃ O(CH₂)₂OMe Br 1-220 CF₃ O(CH₂)₃OMe Br 1-221 CF₃ OCH₂CONMe₂ Br 1-222 CF₃ [1,4]dioxan-2- Br ylmethoxy 1-223 CF₃ O(CH₂)₂OMe I 1-224 CF₃ O(CH₂)₃OMe I 1-225 CF₃ OCH₂CONMe₂ I 1-226 CF₃ [1,4]dioxan-2- I ylmethoxy 1-227 CF₃ F SO₂Me 1-228 CF₃ F SO₂Et 1-229 CF₃ O(CH₂)₂OMe SO₂Me 8.26 (d, 1H), 7.66 (s, 1H), 7.53 (d, 1H), 4.43 (t, 2H), 3.88 (s, 3H), 3.82 (t, 2H), 3.47 (s, 3H), 3.36 (s, 3H) 1-230 CF₃ O(CH₂)₂OMe SO₂Et 1-231 CF₃ O(CH₂)₃OMe SO₂Me 8.05 (d, 1H), 7.42-7.62 (m, 2H), 4.24 (t, 2H), 3.61 (s, 3H). 3.52 (t, 2H), 3.27 (s, 3H), 3.21 (s, 3H), 2.06 (quin, 2H) 1-232 CF₃ O(CH₂)₃OMe SO₂Et 1-233 CF₃ OCH₂CONMe₂ SO₂Me 1-234 CF₃ OCH₂CONMe₂ SO₂Et 1-235 CF₃ [1,4]dioxan-2- SO₂Me ylmethoxy 1-236 CF₃ [1,4]dioxan-2- SO₂Et ylmethoxy 1-237 F Me CF₃ 1-238 F SOMe CF₃ 1-239 Cl Me Cl 2.52 (s, 3H), 3.88 (s, 3H), 7.38 (s, 3H) 1-240 Cl OCH₂CHCH₂ Cl 3.88 (s, 3H), 4.58 (m, 2H), 5.32 (d, 1H), 5.42 (d, 1H), 6.15 (m, 1H), 7.4 (m, 2H), 7.45 (s, 1H) 1-241 Cl OCH₂CHF₂ Cl 3.88 (s, 3H), 4.28 (m, 2H), 6.2 (m, 1H), 7.42 (d, 1H), 7.48 (d, 1H), 7.58 (s, 1H) 1-242 Cl O(CH₂)₂OMe Cl 1-243 Cl OCH₂CONMe₂ Cl 1-244 Cl O(CH₂)-5- Cl pyrrolidin-2-one 1-245 Cl SMe Cl 7.49 (s, 2H), 7.44 (s, 1H), 3.90 (s, 3H), 2.46 (s, 3H) 1-246 Cl SOMe Cl 7.75 (s, 1H), 7.70 (d, 1H), 7.46 (d, 1H), 3.87 (s, 3H), 3.08 (s, 3H) 1-247 Cl SO₂Me Cl 7.65 (d, 1H), 7.64 (s, 1H), 7.56 (d, 1H), 3.86 (s, 3H), 3.35 (s, 3H) 1-248 Cl F SMe 1-249 Cl Cl SO₂Me 3.28 (s, 3H), 3.85 (s, 3H), 7.71 (d, 1H), 7.72 (s, 1H), 8.15 (d, 1H) 1-250 Cl COOMe SO₂Me 1-251 Cl CONMe₂ SO₂Me 1-252 Cl CONMe(OMe) SO₂Me 1-253 Cl CH₂OMe SO₂Me 3.25 (s, 3H), 3.55 (s, 3H), 3.89 (s, 3H), 5.11 (s, 2H), 7.42 (s, 1H), 7.70 (d, 1H), 8.12 (d, 1H) 1-254 Cl CH₂OMe SO₂Et 1-255 Cl CH₂OEt SO₂Me 1.28 (t, 3H), 3.28 (s, 3H), 3.75 (q, 2H), 3.88 (s, 3H), 5.18 (s, 2H), 7.68 (s, 1H), 7.78 (d, 1H), 8.12 (d, 1H) 1-256 Cl CH₂OEt SO₂Et 1-257 Cl CH₂OCH₂CHF₂ SO₂Me 3.22 (s, 3H), 3.88 (m, 2H), 3.88 (s, 3H), 5.31 (s, 2H), 5.95 (m ,1H), 7.52 (s, 1H), 7.75 (d, 1H), 8.15 (d, 1H) 1-258 Cl CH₂OCH₂CF₃ SO₂Me 8.17 (d, 1H), 7.82 (d, 1H), 7.78 (s, 1H), 5.39 (s, 2H), 4.04 (q, 2H), 3.87 (s, 3H), 3.22 (s, 3H) 1-259 Cl CH₂OCH₂CF₃ SO₂Et 1-260 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 3.3 (s, 3H), 3.8 (s, 3H), 4.15 (t, 2H), 5.22 (s, 2H), 6.48 (m, 1H), 7.92 (s, 1H), 7.98 (d, 1H), 8.12 (d, 1H) 1-261 Cl CH₂Ocpentyl SO₂Me 1.48-1.8 (m, 8H), 3.3 (m, 3H), 3.78 (s, 3H), 4.15 (m, 1H), 4.98 (s, 2H), 7.9 (s, 1H), 7.91 (d, 1H), 8.09 (d, 1H) 1.262 Cl CH₂PO(OMe)₂ SO₂Me 3.35 (s, 3H), 3.8 (s, 3H), 3.82 (s, 3H), 4.35 (d, 2H), 7.8 (d, 1H), 7.92 (s, 1H), 8.22 (d, 1H) 1-263 Cl 4,5-dihydro-1,2- SMe 7.81 (s, 1H), 7.72 (d, 1H), oxazol-3-yl 7.24 (d, 1H), 4.59 (t, 2H), 3.93 (s, 3H), 3.31 (t, 2H), 2.51 (s, 3H) 1-264 Cl 4,5-dihydro-1,2- SO₂Me oxazol-3-yl 1-265 Cl 4,5-dihydro-1,2- SO₂Et 8.11 (d, 1H), 7.88 (d, 1H), oxazol-3-yl 7.88 (s, 1H), 4.62 (t, 2H), 3.95 (s, 3H), 3.43 (t, 2H), 3.40 (q, 2H), 1.29 (t, 3H) 1-266 Cl 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol- 3-yl 1-267 Cl 5-cyanomethyl-4,5- SO₂Et 8.09 (d, 1H), 7.92 (d, 1H), dihydro-1,2-oxazol- 7.84 (s, 1H), 5.16 (m, 1H), 3-yl 3.90 (s, 3H), 3.74 (dd, 1H), 3.37 (q, 2H), 3.26 (dd, 1H), 2.90 (dd, 1H), 2.85 (dd, 1H), 1.29 (t, 3H) 1-268 Cl 5-(methoxymethyl)- SO₂Et 1.35 (t, 3H), 3.22 (dd, 1H), 4,5-dihydro-1,2- 3.48 (q, 2H), 3.45 (s, 3H), oxazol-3-yl 3.46 (dd, 1H), 3.6 (dd, 1H), 3.7 (dd, 1H), 3.85 (s, 3H), 5.05 (m, 1H), 7.65 (s, 1H), 7.88 (d, 1H), 8.08 (d, 1H) 1-269 Cl 5-(methoxymethyl)- SO₂Et 1.38 (t, 3H), 1.55 (s, 3H), 3.1 5-methyl-4,5- (d, 1H), 3.4 (q, 2H), 3.45 (m, dihydro-1,2-oxazol- 1H), 3.45 (s, 3H), 3.55 (q, 3-yl 2H), 3.84 (s, 3H), 7.62 (s, 1H), 7.85 (d, 1H), 8.08 (d, 1H) 1-270 Cl CH₂O- SO₂Me 2.02 (m, 2H), 3.3 (s, 3H), 3.7 tetrahydrofuran-3- (m, 2H), 3.78 (m, 2H), 3.78 yl (s, 3H), 4.38 (m, 1H), 5.02 (s, 2H), 7.9 (s, 1H), 7.93 (d, 1H), 8.11 (d, 1H) 1-271 Cl CH₂O-tetra- SO₂Et hydrofuran-3-yl 1-272 Cl CH₂OCH₂- SO₂Me 8.18 (d, 1H), 7.87 (s, 1H), tetrahydrofuran-2- 7.78 (d, 1H), 5.22 (s, 2H), yl 4.15 (m, 1H), 3.95 (s, 3H), 3.88-3.62 (m, 4H), 2.05-1.85 (m, 4H) 1-273 Cl CH₂OCH₂-tetra- SO₂Et hydrofuran-2-yl 1-274 Cl CH₂OCH₂-tetra- SO₂Me 1.5-1.62 (m, 2H), 1.8-2.0 hydrofuran-3-yl (m, 2H), 3.28 (s, 3H), 3.6 (m, 2H), 3.75 (m, 1H), 3.8 (m, 1H), 3.92 (s, 3H), 4.08 (m, 1H), 5.12 (s, 2H), 7.62 (d, 1H), 7.78 (s, 1H), 8.1 (d, 1H) 1-275 Cl CH₂OCH₂-tetra- SO₂Et hydrofuran-3-yl 1-276 Cl OMe SO₂Me 7.97 (d, 1H), 7.80 (s, 1H), 7.63 (d, 1H), 4.11 (s, 3H), 3.87 (s, 3H), 3.26 (s, 3H) 1-277 Cl OMe SO₂Et 11.40 (bs, 1H), 7.92 (bs, 1H), 7.89 (d, 1H), 7.72 (d, 1H), 4.00 (s, 3H), 3.78 (s, 3H), 3.47 (q, 2H), 1.12 (t, 3H) 1-278 Cl OEt SO₂Me 7.99 (d, 1H), 7.84 (s, 1H), 7.57 (d, 1H), 4.34 (q, 2H), 3.93 (s, 3H), 3.28 (s, 3H), 1.53 (t, 3H) 1-279 Cl OEt SO₂Et 11.43 (bs, 1H), 7.92 (bs, 1H), 7.91 (d, 1H), 7.72 (d, 1H), 4.23 (q, 2H), 3.78 (s, 3H), 3.51 (q, 2H), 1.45 (t, 3H), 1.11 (t, 3H) 1-280 Cl OiPr SO₂Me 1-281 Cl OiPr SO₂Et 1-282 Cl O(CH₂)₂OMe SMe 1-283 Cl O(CH₂)₄OMe SO₂Me 1-284 Cl O(CH₂)₄OMe SO₂Et 1-285 Cl O(CH₂)₃OMe SO₂Me 7.98 (d, 1H), 7.82 (s, 1H), 7.58 (d, 1H), 4.35 (t, 2H), 3.92 (s, 3H), 3.63 (t, 2H), 3.38 (s, 3H), 3.27 (s, 3H), 2.20 (quin, 2H) 1-286 Cl O(CH₂)₃OMe SO₂Et 1-287 Cl O(CH₂)₂OMe SO₂Me 1-288 Cl O(CH₂)₂OMe SO₂Et 11.70 (bs, 1H), 7.87-7.92 (m, 2H), 7.71-7.73 (m, 1H), 4.25- 4.33 (m, 4H), 3.79 (s, 3H), 3.53 (q, 2H), 3.36 (s, 3H), 1.13 (t, 3H) 1-289 Cl [1,4]dioxan-2- SO₂Me ylmethoxy 1-290 Cl [1,4]dioxan-2- SO₂Et 7.98 (d, 1H), 7.85 (s, 1H), ylmethoxy 7.60 (d, 1H), 4.36 (dd, 1H), 4.15-4.20 (m, 1H), 4.10-4.15 (m, 1H), 3.65-3.96 (m, 5H), 3.92 (s, 3H), 3.58 (dd, 1H), 3.48 (q, 2H), 1.25 (t, 3H) 1-291 Cl OCH₂(CO)NMe₂ SO₂Me 1-292 Cl OCH₂(CO)NMe₂ SO₂Et 11.45 (bs, 1H), 7.93 (bs, 1H), 7.91 (d, 1H), 7.77 (d, 1H), 4.88 (s, 2H), 3.78 (s, 3H), 3.71 (q, 2H), 2.89 (s, 3H), 2.88 (s, 3H), 1.11 (t, 3H) 1-293 Cl SMe SO₂Me 1-294 Cl SOMe SO₂Me 1-295 Br OMe Br 1-296 Br O(CH₂)₂OMe Br 1-297 Br O(CH₂)₂OMe SO₂Me 1-298 Br O(CH₂)₂OMe SO₂Et 1-299 Br O(CH₂)₃OMe SO₂Me 1-300 Br O(CH₂)₃OMe SO₂Et 1-301 Br O(CH₂)₄OMe SO₂Me 1-302 Br O(CH₂)₄OMe SO₂Et 1-303 Br [1,4]dioxan-2- SO₂Me ylmethoxy 1-304 Br [1,4]dioxan-2- SO₂Et ylmethoxy 1-305 I O(CH₂)₂OMe SO₂Me 1-306 I O(CH₂)₂OMe SO₂Et 1-307 I O(CH₂)₃OMe SO₂Me 1-308 I O(CH₂)₃OMe SO₂Et 1-309 I O(CH₂)₄OMe SO₂Me 1-310 I O(CH₂)₄OMe SO₂Et 1-311 I [1,4]dioxan-2- SO₂Me ylmethoxy 1-312 I [1,4]dioxan-2- SO₂Et ylmethoxy 1-313 OMe SMe CF₃ 8.14 (d, 1H), 7.89 (s, 1H), 7.65 (d, 1H), 4.14 (s, 3H), 3.91 (s, 3H), 2.49 (s, 3H) 1-314 OMe SOMe CF₃ 1-315 OMe SO₂Me CF₃ 8.23 (d, 1H), 7.92 (s, 1H), 7.85 (d, 1H), 4.11 (s, 3H), 3.98 (s, 3H), 3.41 (s, 3H) 1-316 OMe SOEt CF₃ 1-317 OMe SO₂Et CF₃ 1-318 OMe S(CH₂)₂OMe CF₃ 1-319 OMe SO(CH₂)₂OMe CF₃ 1-320 OMe SO₂(CH₂)₂OMe CF₃ 1-321 OMe SMe Cl 1-322 OMe SOMe Cl 1-323 OMe SO₂Me Cl 1-324 OMe SEt Cl 1-325 OMe SOEt Cl 1-326 OMe SO2Et Cl 1-327 OMe S(CH₂)₂OMe Cl 1-328 OMe SO(CH₂)₂OMe Cl 1-329 OMe SO₂(CH₂)₂OMe Cl 1-330 OCH₂c-Pr SMe CF₃ 1-331 OCH₂c-Pr SOMe CF₃ 1-332 OCH₂c-Pr SO₂Me CF₃ 1-333 OCH₂c-Pr SEt CF₃ 1-334 OCH₂c-Pr SOEt CF₃ 1-335 OCH₂c-Pr SO₂Et CF₃ 1-336 OCH₂c-Pr S(CH₂)₂OMe CF₃ 1-337 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 1-338 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 1-339 OCH₂c-Pr SMe Cl 1-340 OCH₂c-Pr SOMe Cl 1-341 OCH₂c-Pr SO₂Me Cl 1-342 OCH₂c-Pr SEt Cl 1-343 OCH₂c-Pr SOEt Cl 1-344 OCH₂c-Pr SO₂Et Cl 1-345 OCH₂c-Pr S(CH₂)₂OMe Cl 1-346 OCH₂c-Pr SO(CH₂)₂OMe Cl 1-347 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 1-348 OCH₂c-Pr SMe SO₂Me 1-349 OCH₂c-Pr SOMe SO₂Me 1-350 OCH₂c-Pr SO₂Me SO₂Me 1-351 OCH₂c-Pr SEt SO₂Me 1-352 OCH₂c-Pr SOEt SO₂Me 1-353 OCH₂c-Pr SO₂Et SO₂Me 1-354 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 1-355 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 1-356 OCH₂c-Pr SO₂ ₍CH₂)₂OMe SO₂Me 1-357 SO₂Me F CF₃ 1-358 SO₂Me NH₂ CF₃ 7.90 (s, 1H), 7.75 (d, 1H), 6.90 (d, 1H), 6.10 (brs, 2H), 4.05 (s, 3H), 3.30 (s, 3H) 1-359 SO₂Me NHEt Cl 1-360 SMe SEt F 1-361 SMe SMe F 1-362 Me F SMe 7.88 (s, 1H), 7.48 (d, 1H), 7.28 (t, 1H), 3.72 (s, 3H), 2.52 (s, 3H), 2.34 (d, 3H) 1-363 Me 1,4-dioxan-2- Cl 10.99 (s, 1H), 7.88 (s, 1H), ylmethoxy 7.46 (d, 1H), 7.37 (d, 1H), 3.86-3.92 (m, 4H), 3.78-3.81 (m, 1H), 3.74 (s, 3H), 3.62- 3.69 (m, 2H), 3.41-3.55 (m, 2H), 2.37 (s, 3H) 1-364 Me tetrahydrofuran-2- Cl 10.98 (s, 1H), 7.88 (s, 1H), ylmethoxy 7.46 (d, 1H), 7.36 (d, 1H), 4.18-4.21 (m, 1H), 3.87-3.90 (m, 2H), 3.74-3.83 (m, 1H), 3.72 (s, 3H), 3.69-3.72 (m, 1H), 2.38 (s, 3H), 1.99-2.04 (m, 1H), 1.84-1.98 (m, 2H), 1.72-1.79 (m, 1H) 1-365 Me SMe SO₂Et 1-366 Me SOMe SO₂Et 1-367 Me SEt SO₂Et 1-368 Me SOEt SO₂Et 1-369 Me SO₂Et SO₂Et 1-370 Me S(CH₂)₂OMe SO₂Et 1-371 Me SO(CH₂)₂OMe SO₂Et 1-372 Me SMe OMe 1-373 Me SOMe OMe 1-374 Me SO₂Me OMe 1-375 Me SEt OMe 1-376 Me SOEt OMe 1-377 Me SO₂Et OMe 1-378 Me S(4-F—Ph) SO₂Me 1-379 Me SO(4-F—Ph) SO₂Me 1-380 Me SO₂(4-F—Ph) SO₂Me 1-381 Me SMe imidazol-1-yl 1-382 Me SMe 1,2,4-triazol-1-yl 1-383 Me SO₂Me imidazol-1-yl 1-384 1-385 Me SOMe 1,2,4-triazol-1-yl 1-386 Me SO₂Me 1,2,4-triazol-1-yl 1-387 Me SMe CN 7.63 (d, 1H), 7.62 (d, 1H), 7.53 (brs, 1H), 3.88 (s, 3H), 2.71 (s, 3H), 2.50 (s, 3H) 1-388 Me SOMe CN 1-389 Me SO₂Me CN 1-390 Me SO₂(CH₂)₂OMe SO₂Et 1-391 Me SMe NMe₂ 1-392 Me SOMe NMe₂ 1-393 Me SO₂Me NMe₂ 1-394 Me SMe OEt 1-395 Me SOMe OEt 1-396 Me SO₂Me OEt 1-397 Me SCH₂CF₃ SO₂Me 1-398 Me SOCH₂CF₃ SO₂Me 1-399 Me SO₂CH₂CF₃ SO₂Me 1-400 Et SOMe CF₃ 1-401 Et SEt CF₃ 1-402 Et SOEt CF₃ 1-403 Et SO₂Et CF₃ 1-404 Et S(CH₂)₂OMe CF₃ 1-405 Et SO(CH₂)₂OMe CF₃ 1-406 Et SO₂(CH₂)₂OMe CF₃ 1-407 Et SOMe Cl 1.22 (t, 3H), 3.10 (s, 3H), 3.10 (m, 1H), 3.25 (m, 1H), 3.95 (s, 3H), 7.4 (d, 1H), 7.6 (d, 1H), 7.93 (s, 1H), 9.98 (br,s, 1H) 1-408 Et SEt Cl 1-409 Et SOEt Cl 1-410 Et SO₂Et Cl 1-411 Et S(CH₂)₂OMe Cl 1-412 Et SO(CH₂)₂OMe Cl 1-413 Et SO₂(CH₂)₂OMe Cl 1-414 Et SEt SO₂Me 1-415 Et SOEt SO₂Me 1-416 Et SO₂Et SO₂Me 1-417 Et S(CH₂)₂OMe SO₂Me 1-418 Et SO(CH₂)₂OMe SO₂Me 1-419 Et SO₂(CH₂)₂OMe SO₂Me 1-420 Et SMe SO₂Et 1-421 Et SOMe SO₂Et 1-422 Et SO₂Me SO₂Et 1-423 Et SEt SO₂Et 1-424 Et SOEt SO₂Et 1-425 Et SO₂Et SO₂Et 1-426 Et S(CH₂)₂OMe SO₂Et 1-427 Et SO(CH₂)₂OMe SO₂Et 1-428 Et SO₂(CH₂)₂OMe SO₂Et 1-429 Et SMe Br 1-430 Et SOMe Br 1-431 Et SO₂Me Br 1-432 Et SMe SO₂Me 1-433 Et SOMe SO₂Me 1-434 Et SO₂Me SO₂Me 1-435 nPr SMe Cl 1-436 nPr SOMe Cl 1-437 nPr SO₂Me Cl 1-438 nPr SMe Br 1-439 nPr SOMe Br 1-440 nPr SO₂Me Br 1-441 nPr SMe CF₃ 0.95 (t, 3H), 1.62 (m, 2H), 2.32 (s, 3H), 3.15 (m, 2H), 3.88 (s, 3H), 7.1 (s, 1H), 7.6 (d, 1H), 7.7 (d, 1H), 11.15 (br,s, 1H) 1-442 nPr SOMe CF₃ 0.98 (t, 3H), 1.55 (m, 1H), 1.72 (m, 1H), 2.98 (s, 3H), 3.35 (m, 1H), 3.62 (m, 1H), 3.9 (s, 3H), 7.55 (s, 1H), 7.68 (d, 1H), 7.72 (d, 1H) 1-443 nPr SO₂Me CF₃ 1-444 nPr SMe SO₂Me 1-445 nPr SOMe SO₂Me 1-446 nPr SO₂Me SO₂Me 1-447 iPr SMe Cl 1.38 (d, 6H), 2.4 (s, 3H), 3.85 (br, s, 1H), 3.9 (s, 3H), 6.98 (s, 1H), 7.35 (d, 1H), 7.45 (d, 1H), 11.2 (br,s, 1H) 1-448 iPr SOMe Cl 1-449 iPr SO₂Me Cl 1-450 iPr SMe Br 1-451 iPr SOMe Br 1-452 iPr SO₂Me Br 1-453 iPr SMe CF₃ 1-454 iPr SOMe CF₃ 1-455 iPr SMe SO₂Me 1-456 iPr SOMe SO₂Me 1-457 iPr SO₂Me SO₂Me 1-458 cPr SMe Cl 1-459 cPr SOMe Cl 1-460 cPr SO₂Me Cl 1-461 cPr SMe Br 1-462 cPr SOMe Br 1-463 cPr SO₂Me Br 1-464 cPr SMe CF₃ 1-465 cPr SOMe CF₃ 1-466 cPr SMe SO₂Me 1-467 cPr SOMe SO₂Me 1-468 cPr SO₂Me SO₂Me 0.62 (br,s, 2H), 1.12 (br,s, 2H), 2.9 (br,s, 1H), 3.52 (s, 3H), 3.65 (s, 3H), 3.9 (s, 3H), 7.7 (br,s, 1H), 7.85 (d, 1H), 8.25 (d, 1H), 11.3 (br,s, 1H) 1-469 CH₂OMe SMe CF₃ 7.86 (s, 2H), 7.80 (s, 1H), 5.14 (s, 2H), 3.91 (s, 3H), 3.59 (s, 3H), 2.39 (s, 3H) 1-470 CH₂OMe SOMe CF₃ 1-471 CH₂OMe SO₂Me CF₃ 1-472 CH₂OMe SEt CF₃ 1-473 CH₂OMe SOEt CF₃ 1-474 CH₂OMe SO₂Et CF₃ 1-475 CH₂OMe S(CH₂)₂OMe CF₃ 1-476 CH₂OMe SO(CH₂)₂OMe CF₃ 1-477 CH₂OMe SO₂(CH₂)₂OMe CF₃ 1-478 CH₂OMe SMe Cl 1-479 CH₂OMe SOMe Cl 1-480 CH₂OMe SO₂Me Cl 1-481 CH₂OMe SEt Cl 1-482 CH₂OMe SOEt Cl 1-483 CH₂OMe SO₂Et Cl 1-484 CH₂OMe S(CH₂)₂OMe Cl 1-485 CH₂OMe SO(CH₂)₂OMe Cl 1-486 CH₂OMe SO₂(CH₂)₂OMe Cl 1-487 CH₂OMe SMe SO₂Me 1-488 CH₂OMe SOMe SO₂Me 1-489 CH₂OMe SO₂Me SO₂Me 1-490 CH₂OMe SEt SO₂Me 1-491 CH₂OMe SOEt SO₂Me 1-492 CH₂OMe SO₂Et SO₂Me 1-493 CH₂OMe S(CH₂)₂OMe SO₂Me 1-494 CH₂OMe SO(CH₂)₂OMe SO₂Me 1-495 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 1-496 CH₂OMe SMe SO₂Et 1-497 CF₃ O(CH₂)₂SMe SO₂Me 8.28 (d, 1H), 7.93 (s, 1H), 7.81 (d, 1H), 4.33 (t, 2H), 3.87 (s, 3H), 3.54 (s, 3H), 2.97 (t, 2H), 2.15 (s, 3H) 1-498 CF₃ tetrahydrofuran-2- SO₂Me 7.88 (s, 1H), 7.79 (d, 1H), ylmethoxy 7.47 (d, 1H), 4.29-4.32 (m, 1H), 3.94-4.03 (m, 2H), 3.83- 3.88 (m, 1H), 3.74-3.79 (m, 1H), 3.77 (s, 3H), 3.23 (s, 3H), 2.41 (s, 3H), 1.91-2.03 (m 1H), 1.85-1.90 (m, 2H), 1.68-1.73 (m, 1H) 1-499 CF₃ OH SO₂Me 11.60 (s, 1H), 8.14 (d, 1H), 7.45 (bd, 1H), 3.90 (s, 3H), 3.40 (s, 3H) 1-500 CF₃ OH SO₂Et 11.70 (s, 1H), 8.12 (d, 1H), 7.46 (d, 1H), 3.98 (s, 3H), 3.52 (q, 2H), 1.15 (t, 3H) 1-501 CF₃ OMe SO₂Me 1-502 CF₃ OEt SO₂Me 8.24 (d, 1H), 7.64 (d, 1H), 4.25 (q, 2H), 3.96 (s, 3H), 3.24 (s, 3H), 1.41 (t, 3H), 1-503 CF₃ O(CH₂)₂OEt SO₂Me 11.40 (bs, 1H), 8.28 (d, 1H), 7.93 (s, 1H), 7.75-7.93 (m, 1H), 4.34 (t, 2H), 3.80 (t, 2H), 3.76 (s, 3H), 3.54 (q, 2H), 3.48 (s, 3H), 1.18 (t, 3H) 1-504 CF₃ O(CH₂)₂SEt SO₂Me 11.45 (s, 1H), 8.28 (d, 1H), 7.94 (s, 1H), 7.81 (d, 1H), 4.31 (t, 2H), 3.76 (s, 3H), 3.47 (s, 3H), 3.00 (t, 2H), 2.60 (q, 2H), 1.22 (t, 3H) 1-505 CF₃ O(CH₂)₃SMe SO₂Me 11.48 (s, 1H), 8.28 (d, 1H), 7.92 (s, 1H), 7.81 (d, 1H), 4.27 (t, 2H), 3.76 (s, 3H), 3.41 (s, 3H), 2.66 (t, 2H), 2.12 (quin, 2H), 2.09 (s, 3H) 1-506 CF₃ OCH₂(CO)N(Me)Et SO₂Me 8.39 (d, 1H), 7.82 (d, 1H), 5.04 (s, 1H), 4.98 (s, 1H), 4.11 (s, 3H), 3.51 (q, 1H), 3.38 (s, 3H), 3.27 (q, 1H), 3.02 (s, 1.5H), 2.94 (s, 1.5H), 1.17-1.22 (m, 3H) 1-507 CF₃ OCH₂(CO)N(Me)Et SO₂Et 8.25 (d, 1H), 7.71 (d, 1H), 4.91 (s, 1H), 4.85 (s, 1H), 3.97 (s, 3H), 3.56 (q, 2H), 3.39 (q, 1H), 3.17 (q, 1H), 3.12 (s, 1.5H), 2.89 (s, 1.5H), 1.05-1.15 (m, 6H) 1-508 CF₃ 2-(2-thienyl)ethoxy SO₂Me 11.49 (bs, 1H), 8.28 (d, 1h), 7.92 (s, 1H), 7.83 (d, 1H), 7.41 (d, 1H), 7.00-7.02 (m, 2H), 4.40 (t, 2H), 3.76 (s, 3H), 3.40 (t, 2H), 3.26 (s, 3H) 1-509 CF₃ 1,3-dioxolan-4- SO₂Me 11.50 (bs, 1H), 8.33 (d, 1H), ylmethoxy 7.93 (s, 1H), 7.81 (d, 1H), 4.85 (d, 1H), 4.75 (d, 1H), 4.50-4.54 (m, 1H), 4.12 (dd, 1H), 3.98 (dd, 1H), 3.76 (s, 3H), 3.47 (s, 3H) 1-510 CF₃ tetrahydro-2H- SO₂Me 11.49 (bs, 1H), 8.29 (d, 1H), pyran-2-ylmethoxy 7.92 (s, 1H), 7.82 (d, 1H), 4.25 (t, 1H), 4.07 (dd, 1H), 3.94 (dd, 1H), 3.76 (s, 3H), 3.48 (s, 3H), 3.41-3.45 (m, 2H), 1.80-1.85 (m, 1H), 1.60- 1.64 (m, 1H), 1.49-1.58 (m, 3H), 1.30-1.34 (m, 1H) 1-511 CF₃ 2-(1H-pyrazol-1- SO₂Me 8.05-8.15 (bs, 1H), 7.68 (d, yl)ethoxy 1H), 7.57 (d, 1H), 7.46 (d, 1H), 6.26 (t, 1H), 4.51-4.57 (m, 4H), 3.76-3.87 (m, 3H), 3.03 (s, 3H) 1-512 CF₃ 2-(1H-pyrazol-1- SO₂Et 12.02 (s, 1H), 8.28 (d, 1H), yl)ethoxy 7.89 (d, 1H), 7.82 (d, 1H), 7.51 (d, 1H), 6.29 (t, 1H), 4.59 (t, 2H), 4.52 (t, 2H), 4.00 (s, 3H), 3.35 (q, 2H), 1.06 (t, 3H) 1-513 CF₃ tetrahydrofuran-2- SO₂Me 8.26 (d, 1H), 7.66 (d, 1H), ylmethoxy 4.34 (dddd, 1H), 4.26 (dd, 1H), 4.11 (dd, 1H), 3.98 (s, 3H), 3.85 (dt, 1H), 3.77 (dt, 1H), 3.32 (s, 3H), 2.03 (dddd, 1H), 1.85-1.92 (m, 2H), 1.69 (dddd, 1H) 1-514 CF₃ tetrahydrofuran-2- SO₂Et 12.01 (s, 1H), 8.30 (d, 1H), ylmethoxy 7.89 (d, 1H), 4.20-4.29 (m, 2H), 4.11 (dd, 1H), 4.00 (s, 3H), 3.80 (dt, 1H), 3.74 (dt, 1H), 3.64 (q, 2H), 2.01 (dddd, 1H), 1.83-1.90 (m, 2H), 1.70 (dddd, 1H), 1.13 (t, 3H) 1-515 CF₃ SMe SO₂Me 12.01 (s, 1H), 8.49 (d, 1H), 8.15 (d, 1H), 4.01 (s, 3H), 3.63 (s, 3H), 2.53 (s, 3H) 1-516 CF₃ SMe SO₂Et 8.43 (d, 1H), 7.90 (d, 1H), 3.96 (s, 3H), 3.70 (q, 2H), 2.46 (s, 3H), 1.12 (t, 3H) 1-517 CF₃ S(O)Me SO₂Me 8.62 (d, 1H), 8.28 (d, 1H), 4.07 (s, 3H), 3.83 (q, 2H), 3.72 (s, 3H), 1.42 (t, 3H) 1-518 CF₃ S(O)₂Me SO₂Me 8.44 (d, 1H), 8.08 (d, 1H), 3.98 (s, 3H), 3.51-3.55 (m, 2H), 3.27 (s, 3H), 1.22 (t, 3H) 1-519 F SCH₂Ph CF3 1-520 F SMe F 1-521 F SOMe F 1-522 F SO₂Me F 1-523 F SEt Cl 7.91 (t, 1H), 7.76 (s, 1H), 7.41 (d, 1H), 3.83 (s, 3H), 2.95 (q, 2H), 1.26 (t, 3H) 1-524 F SOEt Cl 8.07 (dd, 1H), 7.93 (s, 1H), 7.42 (dd, 1H), 3.92 (s, 3H), 3.51 (m, 1H), 3.39 (m, 1H), 1.37 (t, 3H) 1-525 F SO₂Et Cl 8.12 (dd, 1H), 7.95 (s, 1H), 7.53 (dd, 1H), 3.95 (s, 3H), 3.48 (q, 2H), 1.41 (t, 3H) 1-526 Cl SMe H 1-527 Cl SOMe H 1-528 Cl SO₂Me H 1-529 Cl Cl Cl 7.90 (s, 1H), 7.82 (d, 1H), 7.71 (d, 1H), 3.73 (s, 3H) 1-530 Cl SEt Cl 1-531 Cl SOEt Cl 1-532 Cl SO₂Et Cl 1-533 Cl S(CH₂)₂OMe Cl 7.54 (s, 1H), 7.53 (d, 1H), 7.50 (d, 1H), 3.90 (s, 3H), 3.55 (t, 2H), 3.32 (s, 3H), 3.10 (t, 2H) 1-534 Cl SO(CH₂)₂OMe Cl 7.66 (s, 1H), 7.65 (d, 1H), 7.45 (d, 1H), 3.94-3.85 (m, 1H), 3.88 (s, 3H), 3.75 (m, 1H) ,3.66 (m, 1H), 3.40- 3.31 (m, 1H), 3.38 (s, 3H) 1-535 Cl SO₂(CH₂)₂OMe Cl 7.64 (d, 1H), 7.63 (s, 1H), 7.56 (d, 1H), 3.88 (s + t, 5H), 3.71 (t, 2H), 3.23 (s, 3H) 1-536 Cl O(CH₂)₂OEt SO₂Me 7.99 (d, 1H), 7.79 (s, 1H), 7.59 (d, 1H), 4.43-4.45 (m, 2H), 3.89-3.91 (m, 2H), 3.91 (s, 3H), 3.64 (q, 2H), 3.34 (s, 3H), 1.26 (t, 3H) 1-537 Cl O(CH₂)₂OEt SO₂Et 7.97 (d, 1H), 7.73 (s, 1H), 7.60 (d, 1H), 4.42 (t, 2H), 3.89 (t, 2H), 3.89 (s, 3H), 3.64 (q, 2H), 3.52 (q, 2H), 1.27 (t, 3H), 1.25 (t, 3H) 1-538 Cl O(CH₂)₃OCF₃ SO₂Me 7.97 (d, 1H), 7.77 (s, 1H), 7.62 (d, 1H), 4.38 (t, 2H), 4.26 (t, 2H), 3.86 (s, 3H), 3.23 (s, 3H), 2.31 (quin, 2H) 1-539 Cl O(CH₂)₂OCF₃ SO₂Me 7.98 (d, 1H), 7.81 (s, 1H), 7.65 (d, 1H); 4.50-4.52 (m, 2H), 4.41-4.43 (m, 2H), 3.88 (s, 3H), 3.28 (s, 3H) 1-540 Cl O(CH₂)₃OCF₃ SO₂Et 7.96 (d, 1H), 7.74 (s, 1H), 7.61 (d, 1H), 4.36 (t, 2H), 4.25 (t, 2H), 3.88 (s, 3H), 3.38 (q, 2H), 2.30 (quin, 2H), 1.26 (t, 3H) 1-541 Cl O(CH₃)₂OCF₃ SO₂Me 7.96 (d, 1H), 7.73 (s, 1H), 7.65 (d, 1H), 4.48-4.50 (m, 2H), 4.40-4.42 (m, 2H), 3.86 (s, 3H), 3.44 (q, 2H), 1.27 (t, 3H) 1-542 Cl O(CH₂)₂SEt SO₂Me 7.98 (d, 1H), 7.75 (s, 1H), 7.61 (d, 1H), 4.39 (t, 2H), 3.88 (s, 3H), 3.31 (s, 3H), 3.06 (t, 2H), 2.65 (q, 2H), 1.30 (t, 3H) 1-543 Cl O(CH₂)₂SMe SO₂Me 7.98 (d, 1H), 7.74 (s, 1H), 7.61 (d, 1H), 4.41 (t, 2H), 3.88 (s, 3H), 3.31 (s, 3H), 3.02 (t, 2H), 2.22 (s, 3H) 1-544 Cl O(CH₂)₃SMe SO₂Me 7.97 (d, 1H), 7.72 (s, 1H), 7.59 (d, 1H), 4.35 (t, 2H), 3.88 (s, 3H), 3.26 (s, 3H), 2.75 (t, 2H), 2.22 (quin, 2H), 2.16 (s, 3H) 1-545 Cl O(CH₂)₂SMe SO₂Et 7.99 (d, 1H), 7.88 (s, 1H), 7.59 (d, 1H), 4.41 (t, 2H), 3.95 (s, 3H), 3.50 (q, 2H), 3.02 (t, 2H), 2.16 (s, 3H), 1.26 (t, 3H) 1-546 Cl O(CH₂)₃SMe SO₂Et 7.96 (d, 1H), 7.76 (s, 1H), 7.59 (d, 1H), 4.35 (t, 2H), 3.90 (s, 3H), 3.42 (q, 2H), 2.74 (t, 2H), 2.21 (quin, 2H), 2.15 (s, 3H), 1.26 (t, 3H) 1-547 Cl O(CH₂)₂SEt SO₂Et 7.96 (d, 1H), 7.72 (s, 1H), 7.61 (d, 1H), 4.38 (t, 2H), 3.88 (s, 3H), 3.48 (q, 2H), 3.04 (t, 2H), 2.65 (q, 2H), 1.30 (t, 3H), 1.26 (t, 3H) 1-548 Cl OCH₂CN SO₂Et 7.94 (bs, 1H), 7.92 (bs, 1H), 7.82 (bs, 1H), 5.13 (s, 2H), 3.78 (s, 3H), 3.41 (q, 2H), 1.14 (t, 3H) 1-549 Cl OCH₂CH₂F SO₂Me 8.03 (d, 1H), 7.92 (s, 1H), 7.59 (d, 1H), 4.90-4.92 (m, 1H); 4.78-4.80 (m, 1H), 4.57- 4.59 (m, 1H), 4.50-4.52 (m, 1H), 3.97 (s, 3H), 3.92 (s, 3H) 1-550 Cl OCH₂CH₂F SO₂Et 7.97 (d, 1H), 7.73 (s, 1H), 7.65 (d, 1H), 3.89-4.91 (m, 1H), 4.77-4.79 (m, 1H), 4.55- 4.56 (m, 1H), 4.47-4.49 (m, 1H), 3.87 (s, 3H), 3.47 (q, 2H), 1.26 (t, 3H) 1-551 Cl OPr SO₂Et 7.91 (bs, 1H), 7.90 (bd, 1H), 7.70 (bd, 1H), 4.14 (t, 2H), 3.78 (s, 3H), 3.50 (q, 2H), 1.87 (quin, 2H); 1.12 (t, 3H), 1.04 (t, 3H) 1-552 Cl OPr SO₂Me 11.35 (bs, 1H), 7.93 (bs, 1H), 7.92 (d, 1H), 7.69 (d, 1H), 5.15 (t, 2H), 3.78 (s, 3H), 3.37 (s, 3H), 1.89 (quin, 2H), 1.05 (t, 3H) 1-553 Cl propargyloxy SO₂Me 8.02 (d, 1H), 7.93 (bs, 1H), 7.69 (d, 1H), 4.97 (d, 2H), 3.89 (s, 3H), 3.36 (s, 3H), 3.15 (t, 1H) 1-554 Cl propargyloxy SO₂Et 8.00 (d, 1H), 7.94 (s, 1H), 7.70 (d, 1H), 4.96 (bs, 2H), 3.90 (s, 3H), 3.54 (q, 2H), 3.15 (s, 1H), 1.26 (t, 3H) 1-555 Cl allyloxy SO₂Et 11.44 (bs, 1H), 7.92 (d, 1H), 7.75 (d, 1H), 6.18 (m, 1H), 5.50 (d, 1H), 5.36 (d, 1H), 4.69-4.72 (m, 2H), 3.78 (s, 3H), 3.51 (q, 2H), 1.12 (t, 3H) 1-556 Cl allyloxy SO₂Me 11.40 (bs, 1H), 7.94 (d, 1H), 7.74 (d, 1H), 6.20 (m, 1H), 5.52 (d, 1H), 5.36 (d, 1H), 4.69-4.73 (m, 2H), 3.78 (s, 3H), 3.38 (s, 3H) 1-557 Cl SO₂Me SO₂Me 1-558 Cl S(CH₂)₂OMe SO₂Me 1-559 Cl SO(CH₂)₂OMe SO₂Me 1-560 Cl SO₂(CH₂)₂OMe SO₂Me 1-561 Cl SEt SO₂Me 1-562 Cl SOEt SO₂Me 1-563 Cl SO₂Et SO₂Me 1-564 Cl F SOMe 1-565 Cl F SO₂Me 1-566 OH SMe CHF₂ 1-567 OH SO₂Me CHF₂ 1-568 OH SOMe CHF₂ 1-569 OH SCH₂Ph CF3 1-570 OMe SMe OMe 1-571 OMe SOMe OMe 1-572 OMe SO₂Me OMe 1-573 OMe SMe CHF₂ 1-574 OMe SO₂Me CHF₂ 1-575 OMe SOMe CHF₂ 1-576 OMe SMe F 1-577 OMe SOMe F 1-578 OMe SO₂Me F 1-579 OEt SMe CF₃ 1-580 OEt SOMe CF₃ 1-581 OEt SO₂Me CF₃ 1-582 OEt SEt CF₃ 1-583 OEt SOEt CF₃ 1-584 OEt SO₂Et CF₃ 1-585 OEt S(CH₂)₂OMe CF₃ 1-586 OEt SO(CH₂)₂OMe CF₃ 1-587 OEt SO₂(CH₂)₂OMe CF₃ 1-588 OEt SMe Cl 1-589 OEt SOMe Cl 1-590 OEt SO₂Me Cl 1-591 OEt SEt Cl 1-592 OEt SOEt Cl 1-593 OEt SO₂Et Cl 1-594 OEt S(CH₂)₂OMe Cl 1-595 OEt SO(CH₂)₂OMe Cl 1-596 OEt SO₂(CH₂)₂OMe Cl 1-597 SO₂Me NMe₂ Cl 7.78 (s, 1H), 7.66 (d, 1H), 7.40 (d, 1H), 4.05 (s, 3H), 3.35 (s, 3H), 2.93 (s, 6H) 1-598 SO₂Me NHMe Cl 1-599 SO₂Me NH₂ Cl 7.53 (d, 1H), 7.38 (s, 1H), 6.89 (d, 1H), 6.03 (brs, 2H), 3.94 (s, 3H), 3.28 (s, 3H) 1-600 SO₂Me NMe₂ CF₃ 1-601 SO₂Me NHMe CF₃ 1-602 Cl CH₂O(CH₂)₂OMe SO₂Me 3.31 (s, 3H), 3.36 (s, 3H), 3.60 (m, 2H), 3.82 (m, 2H), 3.88 (s, 3H), 5.23 (s, 2H), 7.54 (s, 1H), 7.71 (d, 1H), 8.15 (d, 1H), 11.15 (br, s, 1H) 1-603 Me tetrahydrofuran-2- SO₂Me 7.88 (s, 1H), 7.79 (d, 1H), ylmethoxy 7.47 (d, 1H), 4.29-4.32 (m, 1H), 3.94-4.03 (m, 2H), 3.83- 3.88 (m, 1H), 3.74-3.79 (m, 1H), 3.77 (s, 3H), 3.23 (s, 3H),2.41 (s, 3H), 1.91-2.03 (m, 1H), 1.85-1.90 (m, 2H), 1.68-1.73 (m, 1H) 1-604 CF₃ O(CH₂)₂OMe SO₂Me 8.26 (d, 1H), 7.66 (s, 1H), 7.53 (d, 1H), 4.43 (t, 2H), 3.88 (s, 3H), 3.82 (t, 2H), 3.47 (s, 3H), 3.36 (s, 3H) 1-605 Cl OEt Br 1-606 Cl SMe Me 7.50 (d, 1H), 7.42 (s, 1H), 7.28 (d, 1H), 3.90 (s, 3H), 2.65 (s, 3H), 2.37 (s, 3H) 1-607 CF₃ O(CH₂)₂SMe SO₂Me 8.28 (d, 1H), 7.93 (s, 1H), 7.81 (d, 1H), 4.33 (t, 2H), 3.87 (s, 3H), 3.54 (s, 3H), 2.97 (t, 2H), 2.15 (s, 3H) 1-608 F SEt CF₃ 8.03 (t, 1H), 7.78 (s, 1H), 7.65 (d, 1H), 3.87 (s, 3H), 2.97 (q, 2H), 1.25 (t, 3H) 1-609 F SOEt CF₃ 8.23 (t, 1H), 7.89 (s, 1H), 7.68 (d, 1H), 3.85 (s, 3H), 3.55 (m, 1H), 3.21 (m, 1H), 1.39 (t, 3H) 1-610 F SO₂Et CF₃ 8.37 (t, 1H), 7.87 (s, 1H), 7.83 (d, 1H), 3.85 (s, 3H), 3.46 (q, 2H), 1.42 (t, 3H) 1-611 Cl SCH₂c-Pr Cl 1-612 Cl SOCH₂c-Pr Cl 1-613 Cl SO₂CH₂c-Pr Cl

TABLE 2 Compounds of the formula (I) according to the invention in which A represents CY, B represents CH and R represents ethyl.

Physical data No. X Y Z (¹H-NMR, DMSO-d₆, 400 MHz) 2-1 F H Cl 2-2 F H Br 2-3 F H SO₂Me 2-4 F H SO₂Et 2-5 F H CF₃ 2-6 F H NO₂ 2-7 Cl H F 2-8 Cl H Cl 2-9 Cl H Br 2-10 Cl H SMe 2-11 Cl H SOMe 2-12 Cl H SO₂Me 2-13 Cl H SO₂CH₂Cl 2-14 Cl H SEt 2-15 Cl H SO₂Et 2-16 Cl H CF₃ 2-17 Cl H NO₂ 2-18 Cl H pyrazol-1-yl 2-19 Cl H 1H-1,2,4-triazol- 1-yl 2-20 Br H Cl 2-21 Br H Br 2-22 Br H SO₂Me 2-23 Br H SO₂Et 2-24 Br H CF₃ 2-25 SO₂Me H Cl 2-26 SO₂Me H Br 2-27 SO₂Me H SMe 2-28 SO₂Me H SOMe 2-29 SO₂Me H SO₂Me 2-30 SO₂Me H SO₂Et 2-31 SO₂Me H CF₃ 2-32 SO₂Et H Cl 2-33 SO₂Et H Br 2-34 SO₂Et H SMe 2-35 SO₂Et H SOMe 2-36 SO₂Et H SO₂Me 2-37 SO₂Et H CF₃ 2-38 NO₂ H F 2-39 NO₂ H Cl 2-40 NO₂ H Br 2-41 NO₂ H I 2-42 NO₂ H CN 2-43 NO₂ H SO₂Me 2-44 NO₂ H SO₂Et 2-45 NO₂ H CF₃ 2-46 Me H Cl 2-47 Me H Br 2-48 Me H SMe 2-49 Me H SO₂Me 2-50 Me H SO₂CH₂Cl 2-51 Me H SEt 2-52 Me H SO₂Et 2-53 Me H CF₃ 2-54 CH₂SO₂Me H CF₃ 2-55 Et H Cl 2-56 Et H Br 2-57 Et H SMe 2-58 Et H SO₂Me 2-59 Et H SO₂CH₂Cl 2-60 Et H SEt 2-61 Et H SO₂Et 2-62 Et H CF₃ 2-63 CF₃ H Cl 2-64 CF₃ H Br 2-65 CF₃ H SO₂Me 2-66 CF₃ H SO₂Et 2-67 CF₃ H CF₃ 2-68 NO₂ NH₂ F 2-69 NO₂ NHMe F 2-70 NO₂ NMe₂ F 2-71 NO₂ Me Cl 2-72 NO₂ NH₂ Cl 2-73 NO₂ NHMe Cl 2-74 NO₂ NMe₂ Cl 2-75 NO₂ NH₂ Br 2-76 NO₂ NHMe Br 2-77 NO₂ NMe₂ Br 2-78 NO₂ NH₂ CF₃ 2-79 NO₂ NMe₂ CF₃ 2-80 NO₂ NH₂ SO₂Me 2-81 NO₂ NH₂ SO₂Et 2-82 NO₂ NHMe SO₂Me 2-83 NO₂ NMe₂ SO₂Me 2-84 NO₂ NMe₂ SO₂Et 2-85 NO₂ NH₂ 1H-1,2,4-triazol- 1-yl 2-86 NO₂ NHMe 1H-1,2,4-triazol- 1-yl 2-87 NO₂ NMe₂ 1H-1,2,4-triazol- 1-yl 2-88 Me SMe H 2-89 Me SOMe H 2-90 Me SO₂Me H 2-91 Me SEt H 2-92 Me SOEt H 2-93 Me SO₂Et H 2-94 Me S(CH₂)₂OMe H 2-95 Me SO(CH₂)₂OMe H 2-96 Me SO₂(CH₂)₂OMe H 2-97 Me F F 2-98 Me F Cl 2-99 Me SEt F 2-100 Me SOEt F 2-101 Me SO₂Et F 2-102 Me Me Cl 2-103 Me F Cl 2-104 Me Cl Cl 2-105 Me NH₂ Cl 2-106 Me NHMe Cl 2-107 Me NMe₂ Cl 2-108 Me O(CH₂)₂OMe Cl 2-109 Me O(CH₂)₃OMe Cl 2-110 Me O(CH₂)₄OMe Cl 2-111 Me OCH₂CONMe₂ Cl 2-112 Me O(CH₂)₂—CO—NMe₂ Cl 2-113 Me O(CH₂)₂—NH(CO)NMe₂ Cl 2-114 Me O(CH₂)₂—NH(CO)NHCO₂Et Cl 2-115 Me O(CH₂)₂—NHCO₂Me Cl 2-116 Me O—CH₂—NHSO₂cPr Cl 2-117 Me O(CH₂)-5-2,4- Cl dimethyl-2,4- dihydro-3H-1,2,4- triazol-3-one 2-118 Me O(CH₂)-3,5- Cl dimethyl-1,2-oxazol- 4-yl 2-119 Me SMe Cl 2-120 Me SOMe Cl 2-121 Me SO₂Me Cl 2-122 Me SEt Cl 2-123 Me SOEt Cl 2-124 Me SO₂Et Cl 2-125 Me S(CH₂)₂OMe Cl 2-126 Me SO(CH₂)₂OMe Cl 2-127 Me SO₂(CH₂)₂OMe Cl 2-128 Me NH₂ Br 2-129 Me NHMe Br 2-130 Me NMe₂ Br 2-131 Me O(CH₂)CONEt₂ Br 2-132 Me O(CH₂)-5-pyrrolidin- Br 2-one 2-133 Me SMe Br 2-134 Me SOMe Br 2-135 Me SO₂Me Br 2-136 Me SEt Br 2-137 Me SOEt Br 2-138 Me SO₂Et Br 2-139 Me SMe I 2-140 Me SOMe I 2-141 Me SO₂Me I 2-142 Me SEt I 2-143 Me SOEt I 2-144 Me SO₂Et I 2-145 Me Cl CF₃ 2-146 Me SMe CF₃ 2-147 Me SOMe CF₃ 2-148 Me SO₂Me CF₃ 7.81 (s, 3H), 4.18 (q, 2H), 3.24 (s, 3H), 2.86 (s, 3H), 1.48 (t, 3H) 2-149 Me SEt CF₃ 2-150 Me SOEt CF₃ 2-151 Me SO₂Et CF₃ 2-152 Me S(CH₂)₂OMe CF₃ 2-153 Me SO(CH₂)₂OMe CF₃ 2-154 Me SO₂(CH₂)₂OMe CF₃ 2-155 Me Me SO₂Me 2-156 Me 4,5-dihydro-1,2- SO₂Me oxazol-3-yl 2-157 Me 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 2-158 Me 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol- 3-yl 2-159 Me 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol- 3-yl 2-160 Me NH₂ SO₂Me 2-161 Me NHMe SO₂Me 2-162 Me NMe₂ SO₂Me 2-163 Me NH(CH₂)₂OMe SO₂Me 2-164 Me pyrazol-1-yl SO₂Me 2-165 Me OH SO₂Me 2-166 Me OMe SO₂Me 2-167 Me OMe SO₂Et 2-168 Me OEt SO₂Me 2-169 Me OEt SO₂Et 2-170 Me OiPr SO₂Me 2-171 Me OiPr SO₂Et 2-172 Me O(CH₂)₂OMe SO₂Me 2-173 Me O(CH₂)₂OMe SO₂Et 2-174 Me O(CH₂)₃OMe SO₂Me 2-175 Me O(CH₂)₃OMe SO₂Et 2-176 Me O(CH₂)₄OMe SO₂Me 2-177 Me O(CH₂)₄OMe SO₂Et 2-178 Me O(CH₂)₂NHSO₂Me SO₂Me 2-179 Me O(CH₂)₂NHSO₂Me SO₂Et 2-180 Me OCH₂(CO)NMe₂ SO₂Me 2-181 Me OCH₂(CO)NMe₂ SO₂Et 2-182 Me [1,4]dioxan-2- SO₂Me ylmethoxy 2-183 Me [1,4]dioxan-2- SO₂Et ylmethoxy 2-184 Me O(CH₂)₂—O(3,5-di- SO₂Me methoxypyrimidin-2- yl 2-185 Me Cl SO₂Me 2-186 Me SMe SO₂Me 2-187 Me SOMe SO₂Me 2-188 Me SO₂Me SO₂Me 2-189 Me SO₂Me SO₂Et 2-190 Me SEt SO₂Me 2-191 Me SOEt SO₂Me 2-192 Me SO₂Et SO₂Me 2-193 Me S(CH₂)₂OMe SO₂Me 2-194 Me SO(CH₂)₂OMe SO₂Me 2-195 Me SO₂(CH₂)₂OMe SO₂Me 2-196 CH₂SMe OMe SO₂Me 2-197 CH₂OMe OMe SO₂Me 2-198 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 2-199 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 2-200 CH₂O(CH₂)₃OMe OMe SO₂Me 2-201 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 2-202 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 2-203 Et SMe Cl 2-204 Et SO₂Me Cl 2-205 Et SMe CF₃ 2-206 Et SO₂Me CF₃ 2-207 Et F SO₂Me 2-208 Et NH(CH₂)₂OMe SO₂Me 2-209 iPr SO₂Me CF₃ 2-210 cPr SO₂Me CF₃ 2-211 CF₃ O(CH₂)₂OMe F 2-212 CF₃ O(CH₂)₃OMe F 2-213 CF₃ OCH₂CONMe₂ F 2-214 CF₃ [1,4]dioxan-2- F ylmethoxy 2-215 CF₃ O(CH₂)₂OMe Cl 2-216 CF₃ O(CH₂)₃OMe Cl 2-217 CF₃ OCH₂CONMe₂ Cl 2-218 CF₃ [1,4]dioxan-2- Cl ylmethoxy 2-219 CF₃ O(CH₂)₂OMe Br 2-220 CF₃ O(CH₂)₃OMe Br 2-221 CF₃ OCH₂CONMe₂ Br 2-222 CF₃ [1,4]dioxan-2- Br ylmethoxy 2-223 CF₃ O(CH₂)₂OMe I 2-224 CF₃ O(CH₂)₃OMe I 2-225 CF₃ OCH₂CONMe₂ I 2-226 CF₃ [1,4]dioxan-2- I ylmethoxy 2-227 CF₃ F SO₂Me 2-228 CF₃ F SO₂Et 2-229 CF₃ O(CH₂)₂OMe SO₂Me 2-230 CF₃ O(CH₂)₂OMe SO₂Et 2-231 CF₃ O(CH₂)₃OMe SO₂Me 2-232 CF₃ O(CH₂)₃OMe SO₂Et 2-233 CF₃ OCH₂CONMe₂ SO₂Me 2-234 CF₃ OCH₂CONMe₂ SO₂Et 2-235 CF₃ [1,4]dioxan-2- SO₂Me ylmethoxy 2-236 CF₃ [1,4]dioxan-2- SO₂Et ylmethoxy 2-237 F SMe CF₃ 2-238 F SOMe CF₃ 2-239 Cl Me Cl 2-240 Cl OCH₂CHCH₂ Cl 2-241 Cl OCH₂CHF₂ Cl 2-242 Cl O(CH₂)₂OMe Cl 2-243 Cl OCH₂(CO)NMe₂ Cl 2-244 Cl O(CH₂)-5-pyrrolidin- Cl 2-one 2-245 Cl SMe Cl 2-246 Cl SOMe Cl 2-247 Cl SO₂Me Cl 2-248 Cl F SMe 2-249 Cl Cl SO₂Me 2-250 Cl COOMe SO₂Me 2-251 Cl CONMe₂ SO₂Me 2-252 Cl CONMe(OMe) SO₂Me 2-253 Cl CH₂OMe SO₂Me 2-254 Cl CH₂OMe SO₂Et 2-255 Cl CH₂OEt SO₂Me 2-256 Cl CH₂OEt SO₂Et 2-257 Cl CH₂OCH₂CHF₂ SO₂Me 2-258 Cl CH₂OCH₂CF₃ SO₂Me 2-259 Cl CH₂OCH₂CF₃ SO₂Et 2-260 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 2-261 Cl CH₂Ocpentyl SO₂Me 2-262 Cl CH₂PO(OMe)₂ SO₂Me 2-263 Cl 4,5-dihydro-1,2- SMe oxazol-3-yl 2-264 Cl 4,5-dihydro-1,2- SO₂Me oxazol-3-yl 2-265 Cl 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 2-266 Cl 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol- 3-yl 2-267 Cl 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol- 3-yl 2-268 Cl 5-(methoxymethyl)- SO₂Et 4,5-dihydro-1,2- oxazol-3-yl 2-269 Cl 5-(methoxymethyl)- SO₂Et 5-methyl-4,5-dihy- dro-1,2-oxazol-3-yl 2-270 Cl CH₂O- SO₂Me tetrahydrofuran-3-yl 2-271 Cl CH₂O- SO₂Et tetrahydrofuran-3-yl 2-272 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-2-yl 2-273 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-2-yl 2-274 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-3-yl 2-275 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-3-yl 2-276 Cl OMe SO₂Me 2-277 Cl OMe SO₂Et 2-278 Cl OEt SO₂Me 2-279 Cl OEt SO₂Et 2-280 Cl OiPr SO₂Me 2-281 Cl OiPr SO₂Et 2-282 Cl O(CH₂)₂OMe SO₂Me 2-283 Cl O(CH₂)₄OMe SO₂Me 2-284 Cl O(CH₂)₄OMe SO₂Et 2-285 Cl O(CH₂)₃OMe SO₂Me 2-286 Cl O(CH₂)₃OMe SO₂Et 2-287 Cl O(CH₂)₂OMe SO₂Me 2-288 Cl O(CH₂)₂OMe SO₂Et 2-289 Cl [1,4]dioxan-2- SO₂Me ylmethoxy 2-290 Cl [1,4]dioxan-2- SO₂Et ylmethoxy 2-291 Cl OCH₂(CO)NMe₂ SO₂Me 2-292 Cl OCH₂(CO)NMe₂ SO₂Et 2-293 Cl SMe SO₂Me 2-294 Cl SOMe SO₂Me 2-295 Br OMe Br 2-296 Br O(CH₂)₂OMe Br 2-297 Br O(CH₂)₂OMe SO₂Me 2-298 Br O(CH₂)₂OMe SO₂Et 2-299 Br O(CH₂)₃OMe SO₂Me 2-300 Br O(CH₂)₃OMe SO₂Et 2-301 Br O(CH₂)₄OMe SO₂Me 2-302 Br O(CH₂)₄OMe SO₂Et 2-303 Br [1,4]dioxan-2- SO₂Me ylmethoxy 2-304 Br [1,4]dioxan-2- SO₂Et ylmethoxy 2-305 I O(CH₂)₂OMe SO₂Me 2-306 I O(CH₂)₂OMe SO₂Et 2-307 I O(CH₂)₃OMe SO₂Me 2-308 I O(CH₂)₃OMe SO₂Et 2-309 I O(CH₂)₄OMe SO₂Me 2-310 I O(CH₂)₄OMe SO₂Et 2-311 I [1,4]dioxan-2- SO₂Me ylmethoxy 2-312 I [1,4]dioxan-2- SO₂Et ylmethoxy 2-313 OMe SMe CF₃ 2-314 OMe SOMe CF₃ 2-315 OMe SO₂Me CF₃ 2-316 OMe SOEt CF₃ 2-317 OMe SO₂Et CF₃ 2-318 OMe S(CH₂)₂OMe CF₃ 2-319 OMe SO(CH₂)₂OMe CF₃ 2-320 OMe SO₂(CH₂)₂OMe CF₃ 2-321 OMe SMe Cl 2-322 OMe SOMe Cl 2-323 OMe SO₂Me Cl 2-324 OMe SEt Cl 2-325 OMe SOEt Cl 2-326 OMe SO₂Et Cl 2-327 OMe S(CH₂)₂OMe Cl 2-328 OMe SO(CH₂)₂OMe Cl 2-329 OMe SO₂(CH₂)₂OMe Cl 2-330 OCH₂c-Pr SMe CF₃ 2-331 OCH₂c-Pr SOMe CF₃ 2-332 OCH₂c-Pr SO₂Me CF₃ 2-333 OCH₂c-Pr SEt CF₃ 2-334 OCH₂c-Pr SOEt CF₃ 2-335 OCH₂c-Pr SO₂Et CF₃ 2-336 OCH₂c-Pr S(CH₂)₂OMe CF₃ 2-337 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 2-338 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 2-339 OCH₂c-Pr SMe Cl 2-340 OCH₂c-Pr SOMe Cl 2-341 OCH₂c-Pr SO₂Me Cl 2-342 OCH₂c-Pr SEt Cl 2-343 OCH₂c-Pr SOEt Cl 2-344 OCH₂c-Pr SO₂Et Cl 2-345 OCH₂c-Pr S(CH₂)₂OMe Cl 2-346 OCH₂c-Pr SO(CH₂)₂OMe Cl 2-347 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 2-348 OCH₂c-Pr SMe SO₂Me 2-349 OCH₂c-Pr SOMe SO₂Me 2-350 OCH₂c-Pr SO₂Me SO₂Me 2-351 OCH₂c-Pr SEt SO₂Me 2-352 OCH₂c-Pr SOEt SO₂Me 2-353 OCH₂c-Pr SO₂Et SO₂Me 2-354 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 2-355 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 2-356 OCH₂c-Pr SO₂(CH₂)₂OMe SO₂Me 2-357 SO₂Me F CF₃ 2-358 SO₂Me NH₂ CF₃ 2-359 SO₂Me NHEt Cl 2-360 SMe SEt F 2-361 SMe SMe F 2-362 Me H F 2-363 Me H OCF₃ 2-364 Et H F 2-365 CH₂SO₂Me H Br 2-366 Cl H I 2-367 Cl H CN 2-368 Cl H NMe₂ 2-369 Cl H NHAc 2-370 Cl H pyrrol-1-yl 2-371 Cl H pyrrolidin-1-yl 2-372 Cl H pyrazol-1-yl 2-373 Cl H 1,2,4-triazol-1-yl 2-374 Cl H 4-methyl-3- trifluoromethyl- 1,2,4-triazolin-5- on-1-yl 2-375 Cl H SOMe 2-376 Br H F 2-377 Br H SMe 2-378 NHSO₂Me H CF₃ 2-379 NHSO₂Et H CF₃ 2-380 NHSO2CF₃ H CF₃ 2-381 NHSO₂Me H SO₂Me 2-382 NHSO₂Et H SO₂Me 2-383 NHSO₂CF₃ H SO₂Me 2-384 NMeSO₂Me H CF₃ 2-385 NMeSO₂Et H CF₃ 2-386 NMeSO₂CF₃ H CF₃ 2-387 NMeSO₂Me H SO₂Me 2-388 NMeSO₂Et H SO₂Me 2-389 NMeSO₂CF₃ H SO₂Me 2-390 OMe H SO₂Me 2-391 OSO₂Me H CF₃ 2-392 OSO₂Et H CF₃ 2-393 OSO₂CF₃ H CF₃ 2-394 OSO₂Me H SO₂Me 2-395 OSO₂Et H SO₂Me 2-396 OSO₂CF₃ H SO₂Me 2-397 SMe H CF₃ 2-398 SOMe H CF₃ 2-399 SMe H F 2-400 SMe H Cl 2-401 SMe H Br 2-402 SMe H SMe 2-403 SO₂Me H SO₂Me 2-404 SO₂NMePh H Cl 2-405 SO₂NMe₂ H CF₃ 2-406 Me OMe CF₃ 2-407 Me SMe CN 2-408 Me SOMe CN 2-409 Me SO₂Me CN 2-410 Me Me Cl 2-411 Me O(CH₂)₂N(Me)SO₂Me Cl 2-412 Me O(CH₂)₃SMe Br 2-413 Me O(CH₂)₂SEt Br 2-414 Me O(CH₂)₂SMe Br 2-415 Me O(CH₂)₃SMe Cl 2-416 Me O(CH₂)₂SEt Cl 2-417 Me O(CH₂)2SMe Cl 2-418 Me OEt Cl 2-419 Me OMe Cl 2-420 Me tetrahydrofuran-2- Cl ylmethoxy 2-421 Me 1,4-dioxan-2- Cl ylmethoxy 2-422 Me OEt Cl 2-423 Me OMe Cl 2-424 Me OMe Br 2-425 Me OEt Br 2-426 Me O(CH₂)₂OMe Br 2-427 Me O(CH₂)₃OMe Br 2-428 Me tetrahydrofuran-2- Br ylmethoxy 2-429 Me 1,4-dioxan-2- Br ylmethoxy 2-430 Me SMe NMe₂ 2-431 Me SOMe NMe₂ 2-432 Me SO₂Me NMe₂ 2-433 Me SMe imidazol-1-yl 2-434 Me SMe 1,2,4-triazol-1- yl 2-435 Me SO₂Me imidazol-1-yl 2-436 Me SOMe 1,2,4-triazol-1- yl 2-437 Me SO₂Me 1,2,4-triazol-1- yl 2-438 Me SMe OMe 2-439 Me SOMe OMe 2-440 Me SO₂Me OMe 2-441 Me SEt OMe 2-442 Me SOEt OMe 2-443 Me SO₂Et OMe 2-444 Me SMe OEt 2-445 Me SOMe OEt 2-446 Me SO₂Me OEt 2-447 Me Me SMe 2-448 Me Me SO₂Me 2-449 Me Me SEt 2-450 Me Me SO₂Et 2-451 Me NHiPr SO₂Me 2-452 Me NHCH₂- SO₂Me tetrahydrofuran-2-yl 2-453 Me NHCH₂CONHEt SO₂Me 2-454 Me NH(CH₂)₂OEt SO₂Me 2-455 Me NHEt SO₂Me 2-456 Me NHnPr SO₂Me 2-457 Me NHCH₂iPr SO₂Me 2-458 Me NHCH₂cPr SO₂Me 2-459 Me NHCH₂CH(OMe)CH₂OMe SO₂Me 2-460 Me NHCH₂CH₂CH₂OCOMe SO₂Me 2-461 Me NHCH₂CH₂(1,3- SO₂Me dioxan-2-yl) 2-462 Me NHCH₂Ph SO₂Me 2-463 Me N(CH3)CH₂cPr SO₂Me 2-464 Me NHCH(CH₃)CH₂OMe SO₂Me 2-465 Me NHCH(CH₃)CH₂OEt SO₂Me 2-466 Me NHCH₂CH(OMe)₂ SO₂Me 2-467 Me NHCH₂CH(Me)(OMe) SO₂Me 2-468 Me NHCH₂(1,3-dioxan-2- SO₂Me yl) 2-469 Me 4-Me-pyrazol-1-yl SO₂Me 2-470 Me 3,5-Me₂-pyrazol-1-yl SO₂Me 2-471 Me 4-MeO-pyrazol-1-yl SO₂Me 2-472 Me 4-CN-pyrazol-1-yl SO₂Me 2-473 Me 4-Cl-pyrazol-1-yl SO₂Me 2-474 Me 1,2,3-triazol-1-yl SO₂Me 2-475 Me 1,2,4-triazol-1-yl SO₂Me 2-476 Me 5-iPr-1,2,4-triazol-1- SO₂Me yl 2-477 Me 5-EtS-1,2,4-triazol-1- SO₂Me yl 2-478 Me O(CH₂)₂SMe SO₂Me 2-479 Me O(CH₂)₃SMe SO₂Me 2-480 Me tetrahydrofuran-2- SO₂Me ylmethoxy 2-481 Me F SMe 2-482 Me SMe SO₂Et 2-483 Me SOMe SO₂Et 2-484 Me SEt SO₂Et 2-485 Me SOEt SO₂Et 2-486 Me SO₂Et SO₂Et 2-487 Me SCH₂CF₃ SO₂Me 2-488 Me SOCH₂CF₃ SO₂Me 2-489 Me SO₂CH₂CF₃ SO₂Me 2-490 Me S(CH₂)₂OMe SO₂Et 2-491 Me SO(CH₂)₂OMe SO₂Et 2-492 Me SO₂(CH₂)₂OMe SO₂Et 2-493 Me S(4-F—Ph) SO₂Me 2-494 Me SO(4-F—Ph) SO₂Me 2-495 Me SO₂(4-F—Ph) SO₂Me 2-496 Et SEt Cl 2-497 Et SOEt Cl 2-498 Et SO₂Et Cl 2-499 Et S(CH₂)₂OMe Cl 2-500 Et SO(CH₂)₂OMe Cl 2-501 Et SO₂(CH₂)₂OMe Cl 2-502 Et SOMe Cl 2-503 Et SMe Br 2-504 Et SOMe Br 2-505 Et SO₂Me Br 2-506 Et SOMe CF₃ 2-507 Et SEt CF₃ 2-508 Et SOEt CF₃ 2-509 Et SO₂Et CF₃ 2-510 Et S(CH₂)₂OMe CF₃ 2-511 Et SO(CH₂)₂OMe CF₃ 2-512 Et SO₂(CH₂)₂OMe CF₃ 2-513 Et NHiPr SO₂Me 2-514 Et SMe SO₂Et 2-515 Et SOMe SO₂Et 2-516 Et SO₂Me SO₂Et 2-517 Et SEt SO₂Et 2-518 Et SOEt SO₂Et 2-519 Et SO₂Et SO₂Et 2-520 Et S(CH₂)₂OMe SO₂Et 2-521 Et SO(CH₂)₂OMe SO₂Et 2-522 Et SO₂(CH₂)₂OMe SO₂Et 2-523 Et SEt SO₂Me 2-524 Et SOEt SO₂Me 2-525 Et SO₂Et SO₂Me 2-526 Et S(CH₂)₂OMe SO₂Me 2-527 Et SO(CH₂)₂OMe SO₂Me 2-528 Et SO₂(CH₂)₂OMe SO₂Me 2-529 Et SMe SO₂Me 2-530 Et SOMe SO₂Me 2-531 Et SO₂Me SO₂Me 2-532 nPr SMe Cl 2-533 nPr SOMe Cl 2-534 nPr SO₂Me Cl 2-535 nPr SMe Br 2-536 nPr SOMe Br 2-537 nPr SO₂Me Br 2-538 nPr SMe CF₃ 2-539 nPr SOMe CF₃ 2-540 nPr SO₂Me CF₃ 2-541 nPr SMe SO₂Me 2-542 nPr SOMe SO₂Me 2-543 nPr SO₂Me SO₂Me 2-544 iPr SOMe CF₃ 2-545 iPr SO₂Me CF₃ 2-546 iPr SMe Cl 2-547 iPr SOMe Cl 2-548 iPr SO₂Me Cl 2-549 iPr SMe Br 2-550 iPr SOMe Br 2-551 iPr SO₂Me Br 2-552 iPr SMe SO₂Me 2-553 iPr SOMe SO₂Me 2-554 iPr SO₂Me SO₂Me 2-555 cPr SMe CF₃ 2-556 cPr SOMe CF₃ 2-557 cPr SMe Cl 2-558 cPr SOMe Cl 2-559 cPr SO₂Me Cl 2-560 cPr SMe Br 2-561 cPr SOMe Br 2-562 cPr SO₂Me Br 2-563 cPr SMe SO₂Me 2-564 cPr SOMe SO₂Me 2-565 cPr SO₂Me SO₂Me 2-566 CH₂OMe F CF₃ 2-567 CH₂OMe SMe CF₃ 2-568 CH₂OMe SOMe CF₃ 2-569 CH₂OMe SO₂Me CF₃ 2-570 CH₂OMe SEt CF₃ 2-571 CH₂OMe SOEt CF₃ 2-572 CH₂OMe SO₂Et CF₃ 2-573 CH₂OMe S(CH₂)₂OMe CF₃ 2-574 CH₂OMe SO(CH₂)₂OMe CF₃ 2-575 CH₂OMe SO₂(CH₂)₂OMe CF₃ 2-576 CH₂OMe SMe Cl 2-577 CH₂OMe SOMe Cl 2-578 CH₂OMe SO₂Me Cl 2-579 CH₂OMe SEt Cl 2-580 CH₂OMe SOEt Cl 2-581 CH₂OMe SO₂Et Cl 2-582 CH₂OMe S(CH₂)₂OMe Cl 2-583 CH₂OMe SO(CH₂)₂OMe Cl 2-584 CH₂OMe SO₂(CH₂)₂OMe Cl 2-585 CH₂OMe SMe SO₂Me 2-586 CH₂OMe SOMe SO₂Me 2-587 CH₂OMe SO₂Me SO₂Me 2-588 CH₂OMe SEt SO₂Me 2-589 CH₂OMe SOEt SO₂Me 2-590 CH₂OMe SO₂Et SO₂Me 2-591 CH₂OMe S(CH₂)₂OMe SO₂Me 2-592 CH₂OMe SO(CH₂)₂OMe SO₂Me 2-593 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 2-594 CH₂OMe SMe SO₂Et 2-595 CH₂OMe SOMe SO₂Et 2-596 CH₂OMe SO₂Me SO₂Et 2-597 CH₂OMe SEt SO₂Et 2-598 CH₂OMe SOEt SO₂Et 2-599 CH₂OMe SO₂Et SO₂Et 2-600 CH₂OMe S(CH₂)₂OMe SO₂Et 2-601 CH₂OMe SO(CH₂)₂OMe SO₂Et 2-602 CH₂OMe SO₂(CH₂)₂OMe SO₂Et 2-603 CH₂OMe Cl SO₂Me 2-604 CH₂O(CH₂)₂OEt OEt SO₂Me 2-605 CF₃ SOMe SO₂Me 2-606 CF₃ O(CH₂)₃SMe SO₂Et 2-607 CF₃ O(CH₂)₂OEt SO₂Et 2-608 CF₃ O(CH₂)₂SEt SO₂Et 2-609 CF₃ O(CH₂)₂SMe SO₂Et 2-610 CF₃ O(CH₂)₂OEt SO₂Me 2-611 CF₃ O(CH₂)₂SEt SO₂Me 2-612 CF₃ O(CH₂)₂SMe SO₂Me 2-613 CF₃ O(CH₂)₃SMe SO₂Me 2-614 CF₃ oxetan-3-yloxy SO₂Et 2-615 CF₃ 2-(2-thienyl)ethoxy SO₂Et 2-616 CF₃ 2-(1H-pyrazol-1- SO₂Et yl)ethoxy 2-617 CF₃ 1,3-dioxolan-4- SO₂Et ylmethoxy 2-618 CF₃ tetrahydro-2H-pyran- SO₂Et 2-ylmethoxy 2-619 CF₃ oxetan-3-yloxy SO₂Me 2-620 CF₃ 2-(2-thienyl)ethoxy SO₂Me 2-621 CF₃ 1,3-dioxolan-4- SO₂Me ylmethoxy 2-622 CF₃ tetrahydrofuran-3- SO₂Me ylmethoxy 2-623 CF₃ tetrahydro-2H-pyran- SO₂Me 2-ylmethoxy 2-624 F SO₂Me CF₃ 2-625 F SCH₂Ph CF₃ 2-626 F SMe F 2-627 F SOMe F 2-628 F SO₂Me F 2-629 Cl SO₂Me H 2-630 Cl SCF₂CF₂H H 2-631 Cl SOCF₂CF₂H H 2-632 Cl SO₂CF₂CF₂H H 2-633 Cl SMe Me 2-634 Cl SOMe Me 2-635 Cl SO₂Me Me 2-636 Cl SEt Me 2-637 Cl SOEt Me 2-638 Cl SO₂Et Me 2-639 Cl SMe CF₃ 2-640 Cl SOMe CF₃ 2-641 Cl SO₂Me CF₃ 2-642 Cl CF₃ Cl 2-643 Cl CH₂(4-methyl-3- Cl isopropoxy-1,2,4- triazolin-5-on-1-yl) 2-644 Cl CH₂(4-methyl-3- Cl trifluoroethoxy-1,2,4- triazolin-5-on-1-yl) 2-645 Cl CH₂(4-methyl-3- Cl (methylsulfanyI)-5- oxo-4,5-dihydro-1H- 1,2,4-triazol-1-yl) 2-646 Cl CH₂(4-methyl-3- Cl (methylsulfanyl)-5- oxo-4,5-dihydro-1H- 1,2,4-triazol-1-yl) 2-647 Cl CH₂(3- Cl (dimethylamino)-4- methyl-5-oxo-4,5- dihydro-1H-1,2,4- triazol-1-yl) 2-648 Cl CH₂(3-oxo-5,6,7,8- Cl tetrahydro[1,2,4]triazolo [4,3-a]pyridin- 2(3H)-yl) 2-649 Cl CH₂(4-cyclopropyl-3- Cl methoxy-5-oxo-4,5- dihydro-1H-1,2,4- triazol-1-yl) 2-650 Cl CH₂(3-methyl-6- Cl oxopyridazin-1(6H)- yl) 2-651 Cl CH₂(6-oxopyridazin- Cl 1(6H)-yl) 2-652 Cl CH₂(4-cyclopropyl-5- Cl oxo-3-(2,2,2- trifluoroethoxy)-4,5- dihydro-1H-1,2,4- triazol-1-yl) 2-653 Cl CH₂(3-methoxy-4- Cl methyl-5-oxo-4,5- dihydro-1H-1,2,4- triazol-1-yl) 2-654 Cl CH₂(3,4- Cl dicyclopropyl-5-oxo- 4,5-dihydro-1H-1,2,4- triazol-1-yl) 2-655 Cl CH₂(3-ethoxy-4- Cl methyl-5-oxo-4,5- dihydro-1H-1,2,4- triazol-1-yl) 2-656 Cl NHCH₂CONHEt Cl 2-657 Cl NHCH(CH₃)CONHEt Cl 2-658 Cl NHCH₂CONHiPr Cl 2-659 Cl NHCH(Me)CONH₂ Cl 2-660 Cl NHAc Cl 2-661 Cl NHCON(Me)OMe Cl 2-662 Cl OMe Cl 2-663 Cl OEt Cl 2-664 Cl O(CH₂)₃OMe Cl 2-665 Cl O(CH₂)₃SMe Cl 2-666 Cl O(CH₂)₂SEt Cl 2-667 Cl O(CH₂)₂SMe Cl 2-668 Cl cyclopropylmethoxy Cl 2-669 Cl 1,4-dioxan-2- Cl ylmethoxy 2-670 Cl tetrahydrofuran-2- Cl ylmethoxy 2-671 Cl Br Cl 2-672 Cl SO₂Me Cl 2-673 Cl SOMe Cl 2-674 Cl SMe Cl 2-675 Cl SEt Cl 2-676 Cl SOEt Cl 2-677 Cl SO₂Et Cl 2-678 Cl S(CH₂)₂OMe Cl 2-679 Cl SO(CH₂)₂OMe Cl 2-680 Cl SO₂(CH₂)₂OMe Cl 2-681 Cl 1,4-dioxan-2- Br ylmethoxy 2-682 Cl O(CH₂)₂OMe Br 2-683 Cl tetrahydrofuran-2- Br ylmethoxy 2-684 Cl OCH₂(CO)NMe₂ Br 2-685 Cl O(CH₂)₃OMe Br 2-686 Cl OMe Br 2-687 Cl OEt Br 2-688 Cl Me SMe 2-689 Cl Me SO₂Et 2-690 Cl CH₂N(OMe)Et SO₂Me 2-691 Cl CH₂OC₂H₄OMe SO₂Me 2-692 Cl CH₂OC₂H₄OEt SO₂Me 2-693 Cl CH₂OCH₂iPr SO₂Me 2-694 Cl CH₂OCH₂CF₃ SMe 2-695 Cl CH₂OCH₂cPr SO₂Me 2-696 Cl CO₂H SO₂Me 2-697 Cl NHnPr SO₂Me 2-698 Cl NHCH₂cPr SO₂Me 2-699 Cl NHCH₂CH₂OMe SO₂Me 2-700 Cl NHCH₂CH₂OEt SO₂Me 2-701 Cl NHCH₂CH₂CH₂OMe SO₂Me 2-702 Cl NHCH₂CH₂OCOiPr SO₂Me 2-703 Cl NHCH₂CH₂OCOcPr SO₂Me 2-704 Cl pyrazol-1-yl SO₂Me 2-705 Cl 4-Me-pyrazol-1-yl SO₂Me 2-706 Cl 4-MeO-pyrazol-1-yl SO₂Me 2-707 Cl 4-CN-pyrazol-1-yl SO₂Me 2-708 Cl 4-Cl-pyrazol-1-yl SO₂Me 2-709 Cl 3,5-Me₂-pyrazol-1-yl SO₂Me 2-710 Cl 1,2,4-triazol-1-yl SO₂Me 2-711 Cl 5-iPr-1,2,4-triazol-1- SO₂Me yl 2-712 Cl 5-EtS-1,2,4-triazol- SO₂Me 1-yl 2-713 Cl OPr SO₂Me 2-714 Cl OPr SO₂Et 2-715 Cl isobutoxy SO₂Me 2-716 Cl butoxy SO₂Me 2-717 Cl isohexyloxy SO₂Me 2-718 Cl allyloxy SO₂Me 2-719 Cl allyloxy SO₂Et 2-720 Cl propargyloxy SO₂Et 2-721 Cl propargyloxy SO₂Me 2-722 Cl OCH₂CH₂F SO₂Me 2-723 Cl OCH₂CH₂F SO₂Et 2-724 Cl OCH₂CF₃ SO₂Me 2-725 Cl OCH₂CF₃ SO₂Et 2-726 Cl OCH₂CN SO₂Me 2-727 Cl OCH₂CN SO₂Et 2-728 Cl O(CH₂)₂OEt SO₂Et 2-729 Cl O(CH₂)₂OEt SO₂Me 2-730 Cl O(CH₂)₃OCF₃ SO₂Me 2-731 Cl O(CH₂)₂OCF₃ SO₂Me 2-732 Cl O(CH₂)₃OCF₃ SO₂Et 2-733 Cl O(CH₂)₂OCF₃ SO₂Et 2-734 Cl O(CH₂)₃SEt SO₂Me 2-735 Cl O(CH₂)₃SMe SO₂Et 2-736 Cl O(CH₂)₃SMe SO₂Me 2-737 Cl O(CH₂)₂SEt SO₂Et 2-738 Cl O(CH₂)₂SMe SO₂Et 2-739 Cl O(CH₂)₂SEt SO₂Me 2-740 Cl O(CH₂)₂SMe SO₂Me 2-741 Cl OCH₂(CO)OEt SO₂Et 2-742 Cl OCH₂(CO)OEt SO₂Me 2-743 Cl cyclopropylmethoxy SO₂Et 2-744 Cl cyclopropylmethoxy SO₂Me 2-745 Cl cyclobutylmethoxy SO₂Me 2-746 Cl cyclobutylmethoxy SO₂Et 2-747 Cl 1,3-dioxolan-2- SO₂Me ylmethoxy 2-748 Cl tetrahydro-2H-pyran- SO₂Et 2-ylmethoxy 2-749 Cl tetrahydro-2H-pyran- SO₂Me 2-ylmethoxy 2-750 Cl tetrahydrofuran-3- SO₂Me ylmethoxy 2-751 Cl tetrahydrofuran-3- SO₂Et ylmethoxy 2-752 Cl 3-(1H-tetrazol-1- SO₂Et yl)propoxy 2-753 Cl 3-(2H-tetrazol-2- SO₂Et yl)propoxy 2-754 Cl F SMe 2-755 Cl F SOMe 2-756 Cl F SO₂Me 2-757 Cl SO₂Me SO₂Me 2-758 Cl SEt SO₂Me 2-759 Cl SOEt SO₂Me 2-760 Cl SO₂Et SO₂Me 2-761 Cl S(CH₂)₂OMe SO₂Me 2-762 Cl SO(CH₂)₂OMe SO₂Me 2-763 Cl SO₂(CH₂)₂OMe SO₂Me 2-764 Br SMe Me 2-765 Br SOMe Me 2-766 Br SO₂Me Me 2-767 Br SEt Me 2-768 Br SOEt Me 2-769 Br SO₂Et Me 2-770 Br OEt Br 2-771 Br O(CH₂)₃OMe Br 2-772 Br O(CH₂)₂SMe Br 2-773 Br O(CH₂)₃SMe Br 2-774 Br O(CH₂)₂SEt Br 2-775 Br OCH₂(CO)NMe₂ Br 2-776 Br 1,4-dioxan-2- Br ylmethoxy 2-777 Br tetrahydrofuran-2- Br ylmethoxy 2-778 Br OMe I 2-779 Br OEt I 2-780 Br O(CH₂)₂OMe I 2-781 Br O(CH₂)₃OMe I 2-782 Br 1,4-dioxan-2- I ylmethoxy 2-783 Br tetrahydrofuran-2- I ylmethoxy 2-784 Br OCH₂(CO)NMe₂ I 2-785 Br O(CH₂)₃SMe I 2-786 Br O(CH₂)₂SEt I 2-787 Br O(CH₂)₂SMe I 2-788 Br OMe SO₂Me 2-789 Br OMe SMe 2-790 I SMe Me 2-791 I SOMe Me 2-792 I SO₂Me Me 2-793 I SEt Me 2-794 I SOEt Me 2-795 I SO₂Et Me 2-796 NO₂ SMe Me 2-797 NO₂ SOMe Me 2-798 NO₂ SO₂Me Me 2-799 NO₂ SEt Me 2-800 NO₂ SOEt Me 2-801 NO₂ SO₂Et Me 2-802 NO₂ CH₂OCH₂CF₃ Cl 2-803 NO₂ NMe₂ Cl 2-804 OH SMe CHF₂ 2-805 OH SOMe CHF₂ 2-806 OH SO₂Me CHF₂ 2-807 OH SMe CF₃ 2-808 OH SO₂Me CF₃ 2-809 OH SCH₂Ph CF₃ 2-810 OMe SMe Me 2-811 OMe SOMe Me 2-812 OMe SO₂Me Me 2-813 OMe SMe CHF₂ 2-814 OMe SOMe CHF₂ 2-815 OMe SO₂Me CHF₂ 2-816 OMe SMe OMe 2-817 OMe SOMe OMe 2-818 OMe SO₂Me OMe 2-819 OMe SMe F 2-820 OMe SOMe F 2-821 OMe SO₂Me F 2-822 OMe CH₂N(SO₂Me)Et Cl 2-823 OMe NHCOMe Cl 2-824 OMe NHCOEt Cl 2-825 OMe NHCOiPr Cl 2-826 OMe NHCOcycPr Cl 2-827 OMe NHCOCHCMe₂ Cl 2-828 OMe NHCOPh Cl 2-829 OMe SO₂Me SO₂Me 2-830 OEt SMe CF₃ 2-831 OEt SOMe CF₃ 2-832 OEt SO₂Me CF₃ 2-833 OEt SEt CF₃ 2-834 OEt SOEt CF₃ 2-835 OEt SO₂Et CF₃ 2-836 OEt S(CH₂)₂OMe CF₃ 2-837 OEt SO(CH₂)₂OMe CF₃ 2-838 OEt SO₂(CH₂)₂OMe CF₃ 2-839 OEt SMe Cl 2-840 OEt SOMe Cl 2-841 OEt SO₂Me Cl 2-842 OEt SEt Cl 2-843 OEt SOEt Cl 2-844 OEt SO₂Et Cl 2-845 OEt S(CH₂)₂OMe Cl 2-846 OEt SO(CH₂)₂OMe Cl 2-847 OEt SO₂(CH₂)₂OMe Cl 2-848 OSO₂Me SMe CF₃ 2-849 OSO₂Me SOMe CF₃ 2-850 OSO₂Me SO₂Me CF₃ 2-851 OSO₂Et SMe CF₃ 2-852 OSO₂Et SOMe CF₃ 2-853 OSO₂Et SO₂Me CF₃ 2-854 OSO₂CF₃ SMe CF₃ 2-855 OSO₂CF₃ SOMe CF₃ 2-856 OSO₂CF₃ SO₂Me CF₃ 2-857 SMe SMe H 2-858 SO₂Me SO₂Me H 2-859 SO₂Me SO₂Me Me 2-860 SO₂Me NMe₂ CF₃ 2-861 SO₂Me NHMe CF₃ 2-862 SO₂Me pyrazol-1-yl CF₃ 2-863 SMe OMe F 2-864 SO₂Me OMe F 2-865 SO₂Me NMe₂ Cl 2-866 SO₂Me NHMe Cl 2-867 SO₂Me NH₂ Cl 2-868 SO₂Me NHc-Hex Cl 2-869 SMe OCH₂CHF2 Br 2-870 SO₂Me OMe SO₂Me 2-871 SMe O(CH₂)₃OMe SMe 2-872 SO₂Me F SO₂Me 2-873 SO₂Me SMe SO₂Me 2-874 SO₂Me SO₂Me SO₂Me

TABLE 3 Compounds of the formula (I) according to the invention in which A represents CY, B represents CH and R represents phenyl

Physical data (¹H-NMR, DMSO-d₆, No. X Y Z 400 MHz) 3-1 F H Cl 3-2 F H Br 3-3 F H SO₂Me 3-4 F H SO₂Et 3-5 F H CF₃ 3-6 F H NO₂ 3-7 Cl H F 3-8 Cl H Cl 3-9 Cl H Br 3-10 Cl H SMe 3-11 Cl H SOMe 3-12 Cl H SO₂Me 3-13 Cl H SO₂CH₂Cl 3-14 Cl H SEt 3-15 Cl H SO₂Et 3-16 Cl H CF₃ 3-17 Cl H NO₂ 3-18 Cl H pyrazol-1-yl 3-19 Cl H 1H-1,2,4- triazol-yl 3-20 Br H Cl 3-21 Br H Br 3-22 Br H SO₂Me 3-23 Br H SO₂Et 3-24 Br H CF₃ 3-25 SO₂Me H Cl 3-26 SO₂Me H Br 3-27 SO₂Me H SMe 3-28 SO₂Me H SOMe 3-29 SO₂Me H SO₂Me 3-30 SO₂Me H SO₂Et 3-31 SO₂Me H CF₃ 3-32 SO₂Et H Cl 3-33 SO₂Et H Br 3-34 SO₂Et H SMe 3-35 SO₂Et H SOMe 3-36 SO₂Et H SO₂Me 3-37 SO₂Et H CF₃ 3-38 NO₂ H F 3-39 NO₂ H Cl 3-40 NO₂ H Br 3-41 NO₂ H I 3-42 NO₂ H CN 3-43 NO₂ H SO₂Me 3-44 NO₂ H SO₂Et 3-45 NO₂ H CF₃ 3-46 Me H Cl 3-47 Me H Br 3-48 Me H SMe 3-49 Me H SO₂Me 3-50 Me H SO₂CH₂Cl 3-51 Me H SEt 3-52 Me H SO₂Et 3-53 Me H CF₃ 3-54 CH₂SO₂Me H CF₃ 3-55 Et H Cl 3-56 Et H Br 3-57 Et H SMe 3-58 Et H SO₂Me 3-59 Et H SO₂CH₂Cl 3-60 Et H SEt 3-61 Et H SO₂Et 3-62 Et H CF₃ 3-63 CF₃ H Cl 3-64 CF₃ H Br 3-65 CF₃ H SO₂Me 3-66 CF₃ H SO₂Et 3-67 CF₃ H CF₃ 3-68 NO₂ NH₂ F 3-69 NO₂ NHMe F 3-70 NO₂ NMe₂ F 3-71 NO₂ Me Cl 3-72 NO₂ NH₂ Cl 3-73 NO₂ NHMe Cl 3-74 NO₂ NMe₂ Cl 3-75 NO₂ NH₂ Br 3-76 NO₂ NHMe Br 3-77 NO₂ NMe₂ Br 3-78 NO₂ NH₂ CF₃ 3-79 NO₂ NMe₂ CF₃ 3-80 NO₂ NH₂ SO₂Me 3-81 NO₂ NH₂ SO₂Et 3-82 NO₂ NHMe SO₂Me 3-83 NO₂ NMe₂ SO₂Me 3-84 NO₂ NMe₂ SO₂Et 3-85 NO₂ NH₂ 1H-1,2,4- triazol-1-yl 3-86 NO₂ NHMe 1H-1,2,4- triazol-1-yl 3-87 NO₂ NMe₂ 1H-1,2,4- triazol-1-yl 3-88 Me SMe H 3-89 Me SOMe H 3-90 Me SO₂Me H 3-91 Me SEt H 3-92 Me SOEt H 3-93 Me SO₂Et H 3-94 Me S(CH₂)₂OMe H 3-95 Me SO(CH₂)₂OMe H 3-96 Me SO₂(CH₂)₂OMe H 3-97 Me F F 3-98 Me F Cl 3-99 Me SEt F 3-100 Me SOEt F 3-101 Me SO₂Et F 3-102 Me Me Cl 3-103 Me F Cl 3-104 Me Cl Cl 3-105 Me NH₂ Cl 3-106 Me NHMe Cl 3-107 Me NMe₂ Cl 3-108 Me O(CH₂)₂OMe Cl 3-109 Me O(CH₂)₃OMe Cl 3-110 Me O(CH₂)₄OMe Cl 3-111 Me OCH₂CONMe₂ Cl 3-112 Me O(CH₂)₂—CONMe₂ Cl 3-113 Me O(CH₂)₂—NH(CO)NMe₂ Cl 3-114 Me O(CH₂)₂—NH(CO)NHCO₂Et Cl 3-115 Me O(CH₂)₂NHCO₂Me Cl 3-116 Me OCH₂NHSO₂cPr Cl 3-117 Me O(CH₂)-5-2,4-dimethy1-2,4- Cl dihydro-3H-1,2,4-triazol- 3-one 3-118 Me O(CH₂)-3,5-dimethy1-1,2- Cl oxazol-4-y1 3-119 Me SMe Cl 3-120 Me SOMe Cl 3-121 Me SO₂Me Cl 3-122 Me SEt Cl 3-123 Me SOEt Cl 3-124 Me SO₂Et Cl 3-125 Me S(CH₂)₂OMe Cl 3-126 Me SO(CH₂)₂OMe Cl 3-127 Me SO₂(CH₂)₂OMe Cl 3-128 Me NH₂ Br 3-129 Me NHMe Br 3-130 Me NMe₂ Br 3-131 Me OCH₂CONMe₂ Br 3-132 Me O(CH₂)-5-pyrrolidin-2-one Br 3-133 Me SMe Br 3-134 Me SOMe Br 3-135 Me SO₂Me Br 3-136 Me SEt Br 3-137 Me SOEt Br 3-138 Me SO₂Et Br 3-139 Me SMe I 3-140 Me SOMe I 3-141 Me SO₂Me I 3-142 Me SEt I 3-143 Me SOEt I 3-144 Me SO₂Et I 3-145 Me Cl CF₃ 3-146 Me SMe CF₃ 3-147 Me SOMe CF₃ 3-148 Me SO₂Me CF₃ 7.93 (d, 1 H), 7.91 (s, 1 H), 7.83 (d, 1 H), 7.72-7.65 (m, 5 H), 3.98 (s, 3 H), 3.26 (s, 3 H), 2.83 (s, 3 H) 3-149 Me SEt CF₃ 3-150 Me SOEt CF₃ 3-151 Me SO₂Et CF₃ 3-152 Me S(CH₂)₂OMe CF₃ 3-153 Me SO(CH₂)₂OMe CF₃ 3-154 Me SO₂(CH₂)₂OMe CF₃ 3-155 Me Me SO₂Me 3-156 Me 4,5-dihydro-1,2- SO₂Me oxazol-3-y1 3-157 Me 4,5-dihydro-1,2- SO₂Et oxazol-3-y1 3-158 Me 5-cyanomethy1-4 ,5- SO₂Me dihydro-1,2-oxazol-3-yl 3-159 Me 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol-3-y1 3-160 Me NH₂ SO₂Me 3-161 Me NHMe SO₂Me 3-162 Me NMe₂ SO₂Me 3-163 Me NH(CH₂)₂OMe SO₂Me 3-164 Me pyrazol-1-yl SO₂Me 3-165 Me OH SO₂Me 3-166 Me OMe SO₂Me 3-167 Me OMe SO₂Et 3-168 Me OEt SO₂Me 3-169 Me OEt SO₂Et 3-170 Me OiPr SO₂Me 3-171 Me OiPr SO₂Et 3-172 Me O(CH₂)₂OMe SO₂Me 3-173 Me O(CH₂)₂OMe SO₂Et 3-174 Me O(CH₂)₃OMe SO₂Me 3-175 Me O(CH₂)₃OMe SO₂Et 3-176 Me O(CH₂)₄OMe SO₂Me 3-177 Me O(CH₂)₄OMe SO₂Et 3-178 Me O(CH₂)₂NHSO2Me SO₂Me 3-179 Me O(CH₂)₂NHSO2Me SO₂Et 3-180 Me OCH₂(CO)NMe₂ SO₂Me 3-181 Me OCH₂(CO)NMe₂ SO₂Et 3-182 Me [1,4]dioxan-2- SO₂Me ylmethoxy 3-183 Me [1,4]dioxan-2- SO₂Et ylmethoxy 3-184 Me O(CH₂)₂—O(3,5- SO₂Me dimethoxypyrimidin-2-yl 3-185 Me Cl SO₂Me 3-186 Me SMe SO₂Me 3-187 Me SOMe SO₂Me 3-188 Me SO₂Me SO₂Me 3-189 Me SO₂Me SO₂Et 3-190 Me SEt SO₂Me 3-191 Me SOEt SO₂Me 3-192 Me SO₂Et SO₂Me 3-193 Me S(CH₂)₂OMe SO₂Me 3-194 Me SO(CH₂)₂OMe SO₂Me 3-195 Me SO₂(CH₂)₂OMe SO₂Me 3-196 CH₂SMe OMe SO₂Me 3-197 CH₂OMe OMe SO₂Me 3-198 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 3-199 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 3-200 CH₂O(CH₂)₃OMe OMe SO₂Me 3-201 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 3-202 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 3-203 Et SMe Cl 3-204 Et SO₂Me Cl 3-205 Et SMe CF₃ 3-206 Et SO₂Me CF₃ 3-207 Et F SO₂Me 3-208 Et NH(CH₂)₂OMe SO₂Me 3-209 iPr SO₂Me CF₃ 3-210 cPr SO₂Me CF₃ 3-211 CF₃ O(CH₂)₂OMe F 3-212 CF₃ O(CH₂)₃OMe F 3-213 CF₃ OCH₂CONMe₂ F 3-214 CF₃ [1,4]dioxan-2- F ylmethoxy 3-215 CF₃ O(CH₂)₂OMe Cl 3-216 CF₃ O(CH₂)₃OMe Cl 3-217 CF₃ OCH₂CONMe₂ Cl 3-218 CF₃ [1,4]dioxan-2- Cl ylmethoxy 3-219 CF₃ O(CH₂)₂OMe Br 3-220 CF₃ O(CH₂)₃OMe Br 3-221 CF₃ OCH₂CONMe₂ Br 3-222 CF₃ [1,4]dioxan-2- Br ylmethoxy 3-223 CF₃ O(CH₂)₂OMe I 3-224 CF₃ O(CH₂)₃OMe I 3-225 CF₃ OCH₂CONMe₂ I 3-226 CF₃ [1,4]dioxan-2- I ylmethoxy 3-227 CF₃ F SO₂Me 3-228 CF₃ F SO₂Et 3-229 CF₃ O(CH₂)₂OMe SO₂Me 3-230 CF₃ O(CH₂)₂OMe SO₂Et 3-231 CF₃ O(CH₂)₃OMe SO₂Me 3-232 CF₃ O(CH₂)₃OMe SO₂Et 3-233 CF₃ OCH₂CONMe₂ SO₂Me 3-234 CF₃ OCH₂CONMe₂ SO₂Et 3-235 CF₃ [1,4]dioxan-2- SO₂Me ylmethoxy 3-236 CF₃ [1,4]dioxan-2- SO₂Et ylmethoxy 3-237 F SMe CF₃ 3-238 F SOMe CF₃ 3-239 Cl Me Cl 3-240 Cl OCH₂CHCH₂ Cl 3-241 Cl OCH₂CHF₂ Cl 3-242 Cl O(CH₂)₂OMe Cl 3-243 Cl OCH₂(CO)NMe₂ Cl 3-244 Cl O(CH₂)-5- Cl pyrrolidin-2-one 3-245 Cl SMe Cl 3-246 Cl SOMe Cl 3-247 Cl SO₂Me Cl 3-248 Cl F SMe 3-249 Cl Cl SO₂Me 3-250 Cl COOMe SO₂Me 3-251 Cl CONMe₂ SO₂Me 3-252 Cl CONMe(OMe) SO₂Me 3-253 Cl CH₂OMe SO₂Me 3-254 Cl CH₂OMe SO₂Et 3-255 Cl CH₂OEt SO₂Me 3-256 Cl CH₂OEt SO₂Et 3-257 Cl CH₂OCH₂CHF₂ SO₂Me 3-258 Cl CH₂OCH₂CF₃ SO₂Me 3-259 Cl CH₂OCH₂CF₃ SO₂Et 3-260 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 3-261 Cl CH₂Ocpentyl SO₂Me 3-262 Cl CH₂PO(OMe)₂ SO₂Me 3-263 Cl 4,5-dihydro-1,2-oxazol-3-yl SMe 3-264 Cl 4,5-dihydro-1,2-oxazol-3-yl SO₂Me 3-265 Cl 4,5-dihydro-1,2-oxazol-3-yl SO₂Et 3-266 Cl 5-cyanomethyl-4,5-dihydro- SO₂Me 1,2-oxazol-3-yl 3-267 Cl 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol-3-yl 3-268 Cl 5-(methoxymethyl)-4,5- SO₂Et dihydro-1,2-oxazol-3-y1 3-269 Cl 5-(methoxymethyl)-5- SO₂Et methyl-4,5-dihydro-1,2- oxazol-3-yl 3-270 Cl CH₂O- SO₂Me tetrahydrofuran-3-yl 3-271 Cl CH₂O- SO₂Et tetrahydrofuran-3-yl 3-272 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-2-yl 3-273 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-2-yl 3-274 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-3-yl 3-275 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-3-yl 3-276 Cl OMe SO₂Me 3-277 Cl OMe SO₂Et 3-278 Cl OEt SO₂Me 3-279 Cl OEt SO₂Et 3-280 Cl OiPr SO₂Me 3-281 Cl OiPr SO₂Et 3-282 Cl O(CH₂)₂OMe SO₂Me 3-283 Cl O(CH₂)₄OMe SO₂Me 3-284 Cl O(CH₂)₄OMe SO₂Et 3-285 Cl O(CH₂)₃OMe SO₂Me 3-286 Cl O(CH₂)₃OMe SO₂Et 3-287 Cl O(CH₂)₂OMe SO₂Me 3-288 Cl O(CH₂)₂OMe SO₂Et 3-289 Cl [1,4]dioxan-2-ylmethoxy SO₂Me 3-290 Cl [1,4]dioxan-2-ylmethoxy SO₂Et 3-291 Cl OCH₂(CO)NMe₂ SO₂Me 3-292 Cl OCH₂(CO)NMe₂ SO₂Et 3-293 Cl SMe SO₂Me 3-294 Cl SOMe SO₂Me 3-295 Br OMe Br 3-296 Br O(CH₂)₂OMe Br 3-297 Br O(CH₂)₂OMe SO₂Me 3-298 Br O(CH₂)₂OMe SO₂Et 3-299 Br O(CH₂)₃OMe SO₂Me 3-300 Br O(CH₂)₃OMe SO₂Et 3-301 Br O(CH₂)₄OMe SO₂Me 3-302 Br O(CH₂)₄OMe SO₂Et 3-303 Br [1,4]dioxan-2-ylmethoxy SO₂Me 3-304 Br [1,4]dioxan-2-ylmethoxy SO₂Et 3-305 I O(CH₂)₂OMe SO₂Me 3-306 I O(CH₂)₂OMe SO₂Et 3-307 I O(CH₂)₃OMe SO₂Me 3-308 I O(CH₂)₃OMe SO₂Et 3-309 I O(CH₂)₄OMe SO₂Me 3-310 I O(CH₂)₄OMe SO₂Et 3-311 I [1,4]dioxan-2-ylmethoxy SO₂Me 3-312 I [1,4]dioxan-2-ylmethoxy SO₂Et 3-313 OMe SMe CF₃ 3-314 OMe SOMe CF₃ 3-315 OMe SO₂Me CF₃ 3-316 OMe SOEt CF₃ 3-317 OMe SO₂Et CF₃ 3-318 OMe S(CH₂)₂OMe CF₃ 3-319 OMe SO(CH₂)₂OMe CF₃ 3-320 OMe SO₂(CH₂)₂OMe CF₃ 3-321 OMe SMe Cl 3-322 OMe SOMe Cl 3-323 OMe SO₂Me Cl 3-324 OMe SEt Cl 3-325 OMe SOEt Cl 3-326 OMe SO2Et Cl 3-327 OMe S(CH₂)₂OMe Cl 3-328 OMe SO(CH₂)₂OMe Cl 3-329 OMe SO₂(CH₂)₂OMe Cl 3-330 OCH₂c-Pr SMe CF₃ 3-331 OCH₂c-Pr SOMe CF₃ 3-332 OCH₂c-Pr SO₂Me CF₃ 3-333 OCH₂c-Pr SEt CF₃ 3-334 OCH₂c-Pr SOEt CF₃ 3-335 OCH₂c-Pr SO₂Et CF₃ 3-336 OCH₂c-Pr S(CH₂)₂OMe CF₃ 3-337 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 3-338 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 3-339 OCH₂c-Pr SMe Cl 3-340 OCH₂c-Pr SOMe Cl 3-341 OCH₂c-Pr SO₂Me Cl 3-342 OCH₂c-Pr SEt Cl 3-343 OCH₂c-Pr SOEt Cl 3-344 OCH₂c-Pr SO₂Et Cl 3-345 OCH₂c-Pr S(CH₂)₂OMe Cl 3-346 OCH₂c-Pr SO(CH₂)₂OMe Cl 3-347 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 3-348 OCH₂c-Pr SMe SO₂Me 3-349 OCH₂c-Pr SOMe SO₂Me 3-350 OCH₂c-Pr SO₂Me SO₂Me 3-351 OCH₂c-Pr SEt SO₂Me 3-352 OCH₂c-Pr SOEt SO₂Me 3-353 OCH₂c-Pr SO₂Et SO₂Me 3-354 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 3-355 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 3-356 OCH₂c-Pr SO₂(CH₂)₂OMe SO₂Me 3-357 SO₂Me F CF₃ 3-358 SO₂Me NH₂ CF₃ 3-359 SO₂Me NHEt Cl 3-360 SMe SEt F 3-361 SMe SMe F 3-362 Me H F 3-363 Me H OCF₃ 3-364 Et H F 3-365 CH₂SO₂Me H Br 3-366 Cl H I 3-367 Cl H CN 3-368 Cl H NMe₂ 3-369 Cl H NHAc 3-370 Cl H pyrrol-1-yl 3-371 Cl H pyrrolidin-1-yl 3-372 Cl H pyrazol-1-yl 3-373 Cl H 1,2,4-triazol-1-yl 3-374 Cl H 4-methyl-3- trifluoromethyl- 1,2,4-triazolin-5- on-1-yl 3-375 Cl H SOMe 3-376 Br H F 3-377 Br H SMe 3-378 NHSO₂Me H CF₃ 3-379 NHSO₂Et H CF₃ 3-380 NHSO₂CF₃ H CF₃ 3-381 NHSO₂Me H SO₂Me 3-382 NHSO₂Et H SO₂Me 3-383 NHSO₂CF₃ H SO₂Me 3-384 NMeSO₂Me H CF₃ 3-385 NMeSO₂Et H CF₃ 3-386 NMeSO₂CF₃ H CF₃ 3-387 NMeSO₂Me H SO₂Me 3-388 NMeSO₂Et H SO₂Me 3-389 NMeSO₂CF₃ H SO₂Me 3-390 OMe H SO₂Me 3-391 OSO₂Me H CF₃ 3-392 OSO₂Et H CF₃ 3-393 OSO₂CF₃ H CF₃ 3-394 OSO₂Me H SO₂Me 3-395 OSO₂Et H SO₂Me 3-396 OSO₂CF₃ H SO₂Me 3-397 SMe H CF₃ 3-398 SOMe H CF₃ 3-399 SMe H F 3-400 SMe H Cl 3-401 SMe H Br 3-402 SMe H SMe 3-403 SO₂Me H SO₂Me 3-404 SO₂NMePh H Cl 3-405 SO₂NMe₂ H CF₃ 3-406 Me OMe CF₃ 3-407 Me SMe CN 3-408 Me SOMe CN 3-409 Me SO₂Me CN 3-410 Me Me Cl 3-411 Me O(CH₂)₂N(Me)SO₂Me Cl 3-412 Me O(CH₂)₃SMe Br 3-413 Me O(CH₂)₂SEt Br 3-414 Me O(CH₂)₂SMe Br 3-415 Me O(CH₂)₃SMe Cl 3-416 Me O(CH₂)₂SEt Cl 3-417 Me O(CH₂)₂SMe Cl 3-418 Me OEt Cl 3-419 Me OMe Cl 3-420 Me tetrahydrofuran-2-ylmethoxy Cl 3-421 Me 1,4-dioxan-2-ylmethoxy Cl 3-422 Me OEt Cl 3-423 Me OMe Cl 3-424 Me OMe Br 3-425 Me OEt Br 3-426 Me O(CH₂)₂OMe Br 3-427 Me O(CH₂)₃OMe Br 3-428 Me tetrahydrofuran-2-ylmethoxy Br 3-429 Me 1,4-dioxan-2-ylmethoxy Br 3-430 Me SMe NMe₂ 3-431 Me SOMe NMe₂ 3-432 Me SO₂Me NMe₂ 3-433 Me SMe imidazol-1-yl 3-434 Me SMe 1,2,4-triazol-1-yl 3-435 Me SO₂Me imidazol-1-yl 3-436 Me SOMe 1,2,4-triazol-1-yl 3-437 Me SO₂Me 1,2,4-triazol-1-yl 3-438 Me SMe OMe 3-439 Me SOMe OMe 3-440 Me SO₂Me OMe 3-441 Me SEt OMe 3-442 Me SOEt OMe 3-443 Me SO₂Et OMe 3-444 Me SMe OEt 3-445 Me SOMe OEt 3-446 Me SO₂Me OEt 3-447 Me Me SMe 3-448 Me Me SO₂Me 3-449 Me Me SEt 3-450 Me Me SO₂Et 3-451 Me NHiPr SO₂Me 3-452 Me NHCH₂- SO₂Me tetrahydrofuran-2-yl 3-453 Me NHCH₂CONHEt SO₂Me 3-454 Me NH(CH₂)₂OEt SO₂Me 3-455 Me NHEt SO₂Me 3-456 Me NHnPr SO₂Me 3-457 Me NHCH₂iPr SO₂Me 3-458 Me NHCH₂cPr SO₂Me 3-459 Me NHCH₂CH(OMe)CH₂OMe SO₂Me 3-460 Me NHCH₂CH₂CH₂OCOMe SO₂Me 3-461 Me NHCH₂CH₂(1,3-dioxan-2-yl) SO₂Me 3-462 Me NHCH₂Ph SO₂Me 3-463 Me N(CH₃)CH₂cPr SO₂Me 3-464 Me NHCH(CH₃)CH₂OMe SO₂Me 3-465 Me NHCH(CH₃)CH₂OEt SO₂Me 3-466 Me NHCH₂CH(OMe)₂ SO₂Me 3-467 Me NHCH₂CH(Me)(OMe) SO₂Me 3-468 Me NHCH₂(1,3-dioxan-2-yl) SO₂Me 3-469 Me 4-Me-pyrazol-1-yl SO₂Me 3-470 Me 3,5-Me₂-pyrazol-1-yl SO₂Me 3-471 Me 4-MeO-pyrazol-1-yl SO₂Me 3-472 Me 4-CN-pyrazol-1-yl SO₂Me 3-473 Me 4-Cl-pyrazol-1-yl SO₂Me 3-474 Me 1,2,3-triazol-1-yl SO₂Me 3-475 Me 1,2,4-triazol-1-yl SO₂Me 3-476 Me 5-iPr-1,2,4-triazol-1-yl SO₂Me 3-477 Me 5-EtS-1,2,4-triazol-1-yl SO₂Me 3-478 Me O(CH₂)₂SMe SO₂Me 3-479 Me O(CH₂)₃SMe SO₂Me 3-480 Me tetrahydrofuran-2-ylmethoxy SO₂Me 3-481 Me F SMe 3-482 Me SMe SO₂Et 3-483 Me SOMe SO₂Et 3-484 Me SEt SO₂Et 3-485 Me SOEt SO₂Et 3-486 Me SO₂Et SO₂Et 3-487 Me SCH₂CF₃ SO₂Me 3-488 Me SOCH₂CF₃ SO₂Me 3-489 Me SO₂CH₂CF₃ SO₂Me 3-490 Me S(CH₂)₂OMe SO₂Et 3-491 Me SO(CH₂)₂OMe SO₂Et 3-492 Me SO₂(CH₂)₂OMe SO₂Et 3-493 Me S(4-F—Ph) SO₂Me 3-494 Me SO(4-F—Ph) SO₂Me 3-495 Me SO₂(4-F—Ph) SO₂Me 3-496 Et SEt Cl 3-497 Et SOEt Cl 3-498 Et SO₂Et Cl 3-499 Et S(CH₂)₂OMe Cl 3-500 Et SO(CH₂)₂OMe Cl 3-501 Et SO₂(CH₂)₂OMe Cl 3-502-503 Et SOMe Cl 3-504-505 Et Sme Br 3-506-507 Et SOMe Br 3-508-509 Et SO₂Me Br 3-510-511 Et SOMe CF₃ 3-512 Et SEt CF₃ 3-513 Et SOEt CF₃ 3-514 Et SO₂Et CF₃ 3-515 Et S(CH₂)₂OMe CF₃ 3-516 Et SO(CH₂)₂OMe CF₃ 3-517 Et SO₂(CH₂)₂OMe CF₃ 3-518 Et NHiPr SO₂Me 3-519 Et SMe SO₂Et 3-520 Et SOMe SO₂Et 3-521 Et SO₂Me SO₂Et 3-522 Et SEt SO₂Et 3-523 Et SOEt SO₂Et 3-524 Et SO₂Et SO₂Et 3-525 Et S(CH₂)₂OMe SO₂Et 3-526 Et SO(CH₂)₂OMe SO₂Et 3-527 Et SO₂(CH₂)₂OMe SO₂Et 3-528 Et SEt SO₂Me 3-529 Et SOEt SO₂Me 3-530 Et SO₂Et SO₂Me 3-531 Et S(CH₂)₂OMe SO₂Me 3-532 Et SO(CH₂)₂OMe SO₂Me 3-533 Et SO₂(CH₂)₂OMe SO₂Me 3-534 Et SMe SO₂Me 3-535 Et SOMe SO₂Me 3-536 Et SO₂Me SO₂Me 3-537 nPr SMe Cl 3-538 nPr SOMe Cl 3-539 nPr SO₂Me Cl 3-540 nPr SMe Br 3-541 nPr SOMe Br 3-542 nPr SO₂Me Br 3-543 nPr SMe CF₃ 3-544 nPr SOMe CF₃ 3-545 nPr SO₂Me CF₃ 3-546 nPr SMe SO₂Me 3-547 nPr SOMe SO₂Me 3-548 nPr SO₂Me SO₂Me 3-549 iPr SOMe CF₃ 3-550 iPr SO₂Me CF₃ 3-551 iPr SMe Cl 3-552 iPr SOMe Cl 3-553 iPr SO₂Me Cl 3-554 iPr SMe Br 3-555 iPr SOMe Br 3-556 iPr SO₂Me Br 3-557 iPr SMe SO₂Me 3-558 iPr SOMe SO₂Me 3-559 iPr SO₂Me SO₂Me 3-560 cPr SMe CF₃ 3-561 cPr SOMe CF₃ 3-562 cPr SMe Cl 3-563 cPr SOMe Cl 3-564 cPr SO₂Me Cl 3-565 cPr SMe Br 3-566 cPr SOMe Br 3-567 cPr SO₂Me Br 3-568 cPr SMe SO₂Me 3-569 cPr SOMe SO₂Me 3-570 cPr SO₂Me SO₂Me 3-571 CH₂OMe F CF₃ 3-572 CH₂OMe SMe CF₃ 3-573 CH₂OMe SOMe CF₃ 3-574 CH₂OMe SO₂Me CF₃ 3-575 CH₂OMe SEt CF₃ 3-576 CH₂OMe SOEt CF₃ 3-577 CH₂OMe SO₂Et CF₃ 3-578 CH₂OMe S(CH₂)₂OMe CF₃ 3-579 CH₂OMe SO(CH₂)₂OMe CF₃ 3-580 CH₂OMe SO₂(CH₂)₂OMe CF₃ 3-581 CH₂OMe SMe Cl 3-582 CH₂OMe SOMe Cl 3-583 CH₂OMe SO₂Me Cl 3-584 CH₂OMe SEt Cl 3-585 CH₂OMe SOEt Cl 3-586 CH₂OMe SO₂Et Cl 3-587 CH₂OMe S(CH₂)₂OMe Cl 3-588 CH₂OMe SO(CH₂)₂OMe Cl 3-589 CH₂OMe SO₂(CH₂)₂OMe Cl 3-590 CH₂OMe SMe SO₂Me 3-591 CH₂OMe SOMe SO₂Me 3-592 CH₂OMe SO₂Me SO₂Me 3-593 CH₂OMe SEt SO₂Me 3-594 CH₂OMe SOEt SO₂Me 3-595 CH₂OMe SO₂Et SO₂Me 3-596 CH₂OMe S(CH₂)₂OMe SO₂Me 3-597 CH₂OMe SO(CH₂)₂OMe SO₂Me 3-598 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 3-599 CH₂OMe SMe SO₂Et 3-600 CH₂OMe SOMe SO₂Et 3-601 CH₂OMe SO₂Me SO₂Et 3-602 CH₂OMe SEt SO₂Et 3-603 CH₂OMe SOEt SO₂Et 3-604 CH₂OMe SO₂Et SO₂Et 3-605 CH₂OMe S(CH₂)₂OMe SO₂Et 3-606 CH₂OMe SO(CH₂)₂OMe SO₂Et 3-607 CH₂OMe SO₂(CH₂)₂OMe SO₂Et 3-608 CH₂OMe Cl SO₂Me 3-609 CH₂O(CH₂)₂OEt OEt SO₂Me 3-610 CF₃ SOMe SO₂Me 3-611 CF₃ O(CH₂)₃SMe SO₂Et 3-612 CF₃ O(CH₂)₂OEt SO₂Et 3-613 CF₃ O(CH₂)₂SEt SO₂Et 3-614 CF₃ O(CH₂)₂SMe SO₂Et 3-615 CF₃ O(CH₂)₂OEt SO₂Me 3-616 CF₃ O(CH₂)₂SEt SO₂Me 3-617 CF₃ O(CH₂)₂SMe SO₂Me 3-618 CF₃ O(CH₂)₃SMe SO₂Me 3-619 CF₃ oxetan-3-yloxy SO₂Et 3-620 CF₃ 2-(2-thienyl)ethoxy SO₂Et 3-621 CF₃ 2-(1H-pyrazol-1-yl)ethoxy SO₂Et 3-622 CF₃ 1,3-dioxolan-4-ylmethoxy SO₂Et 3-623 CF₃ tetrahydro-2H-pyran-2- SO₂Et ylmethoxy 3-624 CF₃ oxetan-3-yloxy SO₂Me 3-625 CF₃ 2-(2-thienyl)ethoxy SO₂Me 3-626 CF₃ 1,3-dioxolan-4-ylmethoxy SO₂Me 3-627 CF₃ tetrahydrofuran-3-ylmethoxy SO₂Me 3-628 CF₃ tetrahydro-2H- SO₂Me pyran-2-ylmethoxy 3-629 F SO₂Me CF₃ 3-630 F SCH₂Ph CF₃ 3-631 F SMe F 3-632 F SOMe F 3-633 F SO₂Me F 3-634 Cl SO₂Me H 3-635 Cl SCF₂CF₂H H 3-636 Cl SOCF₂CF₂H H 3-637 Cl SO₂CF₂CF₂H H 3-638 Cl SMe Me 3-639 Cl SOMe Me 3-640 Cl SO₂Me Me 3-641 Cl SEt Me 3-642 Cl SOEt Me 3-643 Cl SO₂Et Me 3-644 Cl SMe CF₃ 3-645 Cl SOMe CF₃ 3-646 Cl SO₂Me CF₃ 3-647 Cl CF₃ Cl 3-648 Cl CH₂(4-methyl-3- Cl isopropoxy-1,2,4- triazolin-5-on-1-y1) 3-649 Cl CH₂(4-methyl-3- Cl trifluoroethoxy-1,2,4- triazolin-5-on-1-y1) 3-650 Cl CH₂(4-methyl-3- Cl (methylsulfany1)-5- oxo-4,5-dihydro-1H- 1,2,4-triazol-1-y1) 3-651 Cl CH₂(4-methyl-3- Cl (methylsulfany1)-5- oxo-4,5-dihydro-1H- 1,2,4-triazol-1-y1) 3-652 Cl CH₂(3-(dimethylamino)-4- Cl methy1-5-oxo-4,5- dihydro-1H-1,2,4-triazol-1-y1) 3-653 Cl CH₂(3-oxo-5,6,7,8-tetrahydro Cl [1,2,4]triazolo[4,3-a]pyridin- 2(3H)-y1) 3-654 Cl CH₂(4-cyclopropyl- Cl 3-methoxy-5-oxo- 4,5-dihydro-1H- 1,2,4-triazol-1-y1) 3-655 Cl CH₂(3-methyl-6- Cl oxopyridazin-1(6H)-yl) 3-656 Cl CH₂(6-oxopyridazin- Cl 1(6H)-yl) 3-657 Cl CH₂(4-cyclopropyl- Cl 5-oxo-3-(2,2,2-trifluoro- ethoxy)-4,5-dihydro- 1H-1,2,4-triazol-1-y1) 3-658 Cl CH₂(3-methoxy-4-methy1-5- Cl oxo-4,5-dihydro-1H-1,2,4- triazol-1-y1) 3-659 Cl CH₂(3,4- Cl dicyclopropy1-5-oxo- 4,5-dihydro-1H- 1,2,4-triazol-1-y1) 3-660 Cl CH₂(3-ethoxy-4- Cl methyl-5-oxo-4,5- dihydro-1H-1,2,4- triazol-1-yl) 3-661 Cl NHCH₂CONHEt Cl 3-662 Cl NHCH(CH₃)CONHEt Cl 3-663 Cl NHCH₂CONHiPr Cl 3-664 Cl NHCH(Me)CONH₂ Cl 3-665 Cl NHAc Cl 3-666 Cl NHCON(Me)OMe Cl 3-667 Cl OMe Cl 3-668 Cl OEt Cl 3-669 Cl O(CH₂)₃OMe Cl 3-670 Cl O(CH₂)₃SMe Cl 3-671 Cl O(CH₂)₂SEt Cl 3-672 Cl O(CH₂)₂SMe Cl 3-673 Cl cyclopropylmethoxy Cl 3-674 Cl 1,4-dioxan-2-ylmethoxy Cl 3-675 Cl tetrahydrofuran-2- ylmethoxy Cl 3-676 Cl Br Cl 3-677 Cl SO₂Me Cl 3-678 Cl SOMe Cl 3-679 Cl SMe Cl 3-680 Cl SEt Cl 3-681 Cl SOEt Cl 3-682 Cl SO₂Et Cl 3-683 Cl S(CH₂)₂OMe Cl 3-684 Cl SO(CH₂)₂OMe Cl 3-685 Cl SO₂(CH₂)₂OMe Cl 3-686 Cl 1,4-dioxan-2-ylmethoxy Br 3-687 Cl O(CH₂)₂OMe Br 3-688 Cl tetrahydrofuran-2-ylmethoxy Br 3-689 Cl OCH₂(CO)NMe₂ Br 3-690 Cl O(CH₂)₃OMe Br 3-691 Cl OMe Br 3-692 Cl OEt Br 3-693 Cl Me SMe 3-694 Cl Me SO₂Et 3-695 Cl CH₂N(OMe)Et SO₂Me 3-696 Cl CH₂OC₂H₄OMe SO₂Me 3-697 Cl CH₂OC₂H₄OEt SO₂Me 3-698 Cl CH₂OCH₂iPr SO₂Me 3-699 Cl CH₂OCH₂CF₃ SMe 3-700 Cl CH₂OCH₂cPr SO₂Me 3-701 Cl CO₂H SO₂Me 3-702 Cl NHnPr SO₂Me 3-703 Cl NHCH₂cPr SO₂Me 3-704 Cl NHCH₂CH₂OMe SO₂Me 3-705 Cl NHCH₂CH₂OEt SO₂Me 3-706 Cl NHCH₂CH₂CH₂OMe SO₂Me 3-707 Cl NHCH₂CH₂OCOiPr SO₂Me 3-708 Cl NHCH₂CH₂OCOcPr SO₂Me 3-709 Cl pyrazol-1-yl SO₂Me 3-710 Cl 4-Me-pyrazol-1-yl SO₂Me 3-711 Cl 4-MeO-pyrazol-1-yl SO₂Me 3-712 Cl 4-CN-pyrazol-1-yl SO₂Me 3-713 Cl 4-Cl-pyrazol-1-yl SO₂Me 3-714 Cl 3,5-Me₂-pyrazol-1-yl SO₂Me 3-715 Cl 1,2,4-triazol-1-yl SO₂Me 3-716 Cl 5-iPr-1,2,4-triazol-1-yl SO₂Me 3-717 Cl 5-EtS-1,2,4-triazol-1-yl SO₂Me 3-718 Cl OPr SO₂Me 3-719 Cl OPr SO₂Et 3-720 Cl isobutoxy SO₂Me 3-721 Cl butoxy SO₂Me 3-722 Cl isohexyloxy SO₂Me 3-723 Cl allyloxy SO₂Me 3-724 Cl allyloxy SO₂Et 3-725 Cl propargyloxy SO₂Et 3-726 Cl propargyloxy SO₂Me 3-727 Cl OCH₂CH₂F SO₂Me 3-728 Cl OCH₂CH₂F SO₂Et 3-729 Cl OCH₂CF₃ SO₂Me 3-730 Cl OCH₂CF₃ SO₂Et 3-731 Cl OCH₂CN SO₂Me 3-732 Cl OCH₂CN SO₂Et 3-733 Cl O(CH₂)₂OEt SO₂Et 3-734 Cl O(CH₂)₂OEt SO₂Me 3-735 Cl O(CH₂)₃OCF₃ SO₂Me 3-736 Cl O(CH₂)₂OCF₃ SO₂Me 3-737 Cl O(CH₂)₃OCF₃ SO₂Et 3-738 Cl O(CH₂)₂OCF₃ SO₂Et 3-739 Cl O(CH₂)₃SEt SO₂Me 3-740 Cl O(CH₂)₃SMe SO₂Et 3-741 Cl O(CH₂)₃SMe SO₂Me 3-742 Cl O(CH₂)₂SEt SO₂Et 3-743 Cl O(CH₂)₂SMe SO₂Et 3-744 Cl O(CH₂)₂SEt SO₂Me 3-745 Cl O(CH₂)₂SMe SO₂Me 3-746 Cl OCH₂(CO)OEt SO₂Et 3-747 Cl OCH₂(CO)OEt SO₂Me 3-748 Cl cyclopropylmethoxy SO₂Et 3-749 Cl cyclopropylmethoxy SO₂Me 3-750 Cl cyclobutylmethoxy SO₂Me 3-751 Cl cyclobutylmethoxy SO₂Et 3-752 Cl 1,3-dioxolan-2-ylmethoxy SO₂Me 3-753 Cl tetrahydro-2H- SO₂Et pyran-2-ylmethoxy 3-754 Cl tetrahydro-2H- SO₂Me pyran-2-ylmethoxy 3-755 Cl tetrahydrofuran-3-ylmethoxy SO₂Me 3-756 Cl tetrahydrofuran-3-ylmethoxy SO₂Et 3-757 Cl 3-(1H-tetrazol-1-yl)propoxy SO₂Et 3-758 Cl 3-(2H-tetrazol-2-yl)propoxy SO₂Et 3-759 Cl F SMe 3-760 Cl F SOMe 3-761 Cl F SO₂Me 3-762 Cl SO₂Me SO₂Me 3-763 Cl SEt SO₂Me 3-764 Cl SOEt SO₂Me 3-765 Cl SO₂Et SO₂Me 3-766 Cl S(CH₂)₂OMe SO₂Me 3-767 Cl SO(CH₂)₂OMe SO₂Me 3-768 Cl SO₂(CH₂)₂OMe SO₂Me 3-769 Br SMe Me 3-770 Br SOMe Me 3-771 Br SO₂Me Me 3-772 Br SEt Me 3-773 Br SOEt Me 3-774 Br SO₂Et Me 3-775 Br OEt Br 3-776 Br O(CH₂)₃OMe Br 3-777 Br O(CH₂)₂SMe Br 3-778 Br O(CH₂)₃SMe Br 3-779 Br O(CH₂)₂SEt Br 3-780 Br OCH₂(CO)NMe₂ Br 3-781 Br 1,4-dioxan-2-ylmethoxy Br 3-782 Br tetrahydrofuran-2-ylmethoxy Br 3-783 Br OMe I 3-784 Br OEt I 3-785 Br O(CH₂)₂OMe I 3-786 Br O(CH₂)₃OMe I 3-787 Br 1,4-dioxan-2- I ylmethoxy 3-788 Br tetrahydrofuran-2-ylmethoxy I 3-789 Br OCH₂(CO)NMe₂ I 3-790 Br O(CH₂)₃SMe I 3-791 Br O(CH₂)₂SEt I 3-792 Br O(CH₂)₂SMe I 3-793 Br OMe SO₂Me 3-794 Br OMe SMe 3-795 I SMe Me 3-796 I SOMe Me 3-797 I SO₂Me Me 3-798 I SEt Me 3-799 I SOEt Me 3-800 I SO₂Et Me 3-801 NO₂ SMe Me 3-802 NO₂ SOMe Me 3-803 NO₂ SO₂Me Me 3-804 NO₂ SEt Me 3-805 NO₂ SOEt Me 3-806 NO₂ SO₂Et Me 3-807 NO₂ CH₂OCH₂CF₃ Cl 3-808 NO₂ NMe₂ Cl 3-809 OH SMe CHF₂ 3-810 OH SOMe CHF₂ 3-811 OH SO₂Me CHF₂ 3-812 OH SMe CF₃ 3-813 OH SO₂Me CF₃ 3-814 OH SCH₂Ph CF₃ 3-815 OMe SMe Me 3-816 OMe SOMe Me 3-817 OMe SO₂Me Me 3-818 OMe SMe CHF₂ 3-819 OMe SOMe CHF₂ 3-820 OMe SO₂Me CHF₂ 3-821 OMe SMe OMe 3-822 OMe SOMe OMe 3-823 OMe SO₂Me OMe 3-824 OMe SMe F 3-825 OMe SOMe F 3-826 OMe SO₂Me F 3-827 OMe CH₂N(SO₂Me)Et Cl 3-828 OMe NHCOMe Cl 3-829 OMe NHCOEt Cl 3-830 OMe NHCOiPr Cl 3-831 OMe NHCOcycPr Cl 3-832 OMe NHCOCHCMez Cl 3-833 OMe NHCOPh Cl 3-834 OMe SO₂Me SO₂Me 3-835 OEt SMe CF₃ 3-836 OEt SOMe CF₃ 3-837 OEt SO₂Me CF₃ 3-838 OEt SEt CF₃ 3-839 OEt SOEt CF₃ 3-840 OEt SO₂Et CF₃ 3-841 OEt S(CH₂)₂OMe CF₃ 3-842 OEt SO(CH₂)₂OMe CF₃ 3-843 OEt SO₂(CH₂)₂OMe CF₃ 3-844 OEt SMe Cl 3-845 OEt SOMe Cl 3-846 OEt SO₂Me Cl 3-847 OEt SEt Cl 3-848 OEt SOEt Cl 3-849 OEt SO₂Et Cl 3-850 OEt S(CH₂)₂OMe Cl 3-851 OEt SO(CH₂)₂OMe Cl 3-852 OEt SO₂(CH₂)₂OMe Cl 3-853 OSO₂Me SMe CF₃ 3-854 OSO₂Me SOMe CF₃ 3-855 OSO₂Me SO₂Me CF₃ 3-856 OSO₂Et SMe CF₃ 3-857 OSO₂Et SOMe CF₃ 3-858 OSO₂Et SO₂Me CF₃ 3-859 OSO₂CF₃ SMe CF₃ 3-860 OSO₂CF₃ SOMe CF₃ 3-861 OSO₂CF₃ SO₂Me CF₃ 3-862 SMe SMe H 3-863 SO₂Me SO₂Me H 3-864 SO₂Me SO₂Me Me 3-865 SO₂Me NMe₂ CF₃ 3-866 SO₂Me NHMe CF₃ 3-867 SO₂Me pyrazol-1-yl CF₃ 3-868 SMe OMe F 3-869 SO₂Me OMe F 3-870 SO₂Me NMe₂ Cl 3-871 SO₂Me NHMe Cl 3-872 SO₂Me NH₂ Cl 3-873 SO₂Me NHc-Hex Cl 3-874 SMe OCH₂CHF₂ Br 3-875 SO₂Me OMe SO₂Me 3-876 SMe O(CH₂)₃OMe SMe 3-877 SO₂Me F SO₂Me 3-878 SO₂Me SMe SO₂Me 3-879 SO₂Me SO₂Me SO₂Me

TABLE 4 Compounds of the formula (I) according to the invention in which A represents CY, B represents N and R represents methyl

Physical data No. X Y Z (¹H-NMR, DMSO-d₆, 400 MHz) 4-1 F H Cl 4-2 F H Br 4-3 F H SO₂Me 11.83 (brs, 1 H), 8.07 (t, 1 H), 8.01 (dd, 1 H), 7.94 (dd, 1 H), 3.98 (s, 3 H), 3.36 (s, 3 H) 4-4 F H SO₂Et 4-5 F H CF₃ 4-6 Cl H F 4-7 Cl H Cl 9.70 (brs), 7.83 (d, 1 H), 7.55 (d, 1 H), 7.44 (dd, 1 H), 4.10 (s, 3 H) 4-8 Cl H Br 7.94 (d, 1 H), 7.75 (dd, 1 H), 7.71 (d, 1 H), 3.99 (s, 3 H) 4-9 Cl H SMe 7.66 (d, 1 H), 7.45 (d, 1 H), 7.36 (dd, 1 H), 3.97 (s, 3 H), 2.56 (s, 3 H) 4-10 Cl H SO₂Me 8.12 (s, 1 H), 8.01 (s, 2 H), 4.12 (s, 3 H), 3.13 (s, 3 H) 4-11 Cl H SO₂CH₂Cl 4-12 Cl H Set 7.82 (d, 1 H), 7.32 (m, 1 H), 7.12 (m, 1 H), 4.09 (s, 3 H), 3.02 (q, 2 H), 1.40 (t, 3 H) 4-13 Cl H SO₂Et 8.11 (s, 1 H), 8.04 (d, 1 H), 8.01 (d, 1 H), 4.02 (s, 3 H), 3.47 (q, 2 H), 1.14 (t, 3 H) 4-14 Cl H CF₃ 8.00 (s, 1 H), 7.92 (d, 1 H), 7.85 (d, 1 H), 3.94 (s, 3 H) 4-15 Br H Cl 4-16 Br H Br 8.07 (s, 1 H), 7.78 (d, 2 H), 7.68 (d, 1 H), 4.00 (s, 3 H) 4-17 Br H SO₂Me 8.26 (s, 1 H), 8.02 (d, 2 H), 7.86 (d, 1 H), 4.11 (s, 3 H), 3.12 (s, 3 H) 4-18 Br H SO₂Et 4-19 Br H CF₃ 10.95 (brs), 7.97 (s, 1 H), 7.85 (d, 1 H), 7.75 (dd, 1 H), 4.15 (s, 3 H) 4-20 SO₂Me H Cl 8.05 (s, 1 H), 8.02 (d, 1 H), 7.95 (d, 1 H), 4.02 (s, 3 H), 3.42 (s, 3 H) 4-21 SO₂Me H Br 4-22 SO₂Me H SMe 4-23 SO₂Me H SOMe 4-24 SO₂Me H SO₂Me 4-25 SO₂Me H CF₃ 8.41 (s, 1 H), 8.07 (d, 1 H), 8.00 (d, 1 H), 4.19 (s, 3 H), 3.37 (s, 3 H) 4-26 SO₂Et H Cl 4-27 SO₂Et H Br 4-28 SO₂Et H SMe 4-29 SO₂Et H SOMe 4-30 SO₂Et H SO₂Me 4-31 SO₂Et H CF₃ 4-32 NO₂ H F 4-33 NO₂ H Cl 8.15 (s, 1 H), 7.79 (d, 2 H), 7.73 (d, 1 H), 4.18 (s, 3 H) 4-34 NO₂ H Br 12.04 (brs, 1 H), 8.45 (d, 1 H), 8.18 (d, 1 H), 7.88 (brd, 1 H), 4.00 (s, 3 H) 4-35 NO₂ H I 12.0 (brs, 1 H), 8.53 (d, 1 H), 8.31 (d, 1 H), 7.68 (brd, 1 H), 3.99 (s, 3 H) 4-36 NO₂ H CN 12.15 (brs, 1 H), 8.82 (s, 1 H), 8.45 (d, 1 H), 8.16 (brs, 1 H), 4.02 (s, 3 H) 4-37 NO₂ H SO₂Me 8.68 (s, 1 H), 8.47 (d, 1 H), 8.23 (m, 1 H), 4.03 (s, 3 H), 3.43 (s, 3 H) 4-38 NO₂ H SO₂Et 4-39 NO₂ H CF₃ 8.58 (s, 1 H), 8.37 (d, 1 H), 8.18 (m, 1 H), 4.02 (s, 3 H) 4-40 Me H Cl 7.69 (d, 1 H), 7.48 (d, 1 H), 7.44 (dd, 1 H), 3.97 (s, 3 H), 2.44 (s, 3 H) 4-41 Me H Br 4-42 Me H SO₂Me 7.94 (s, 1 H), 7.89 (s, 2 H), 4.00 (s, 3 H), 3.42 (s, 3 H), 2.51 (s, 3 H) 4-43 Me H SO₂CH₂Cl 4-44 Me H SO₂Et 4-45 Me H CF₃ 4-46 CH₂SO₂Me H CF₃ 11.81 (brs, 1 H), 7.94 (d, 1 H), 7.86 (s, 1 H), 7.83 (d, 1 H), 4.04 (s, 2 H), 4.02 (s, 3 H), 1.95 (s, 3 H) 4-47 Et H Cl 11.56 (brs, 1 H), 7.68 (d, 1 H), 7.48 (d, 1 H), 7.44 (dd, 1 H), 3.97 (s, 3 H), 2.78 (q, 2 H), 1.18 (t, 3 H) 4-48 Et H Br 7.62 (s, 1 H), 7.60 (d, 1 H), 7.57 (dd, 1 H), 3.97 (s, 3 H), 2.77 (q, 2 H), 1.18 (t, 3 H) 4-49 Et H SO₂Me 4-50 Et H SO₂CH₂Cl 4-51 Et H SEt 4-52 Et H SO₂Et 4-53 Et H CF₃ 4-54 CF₃ H Cl 11.93 (brs), 8.03 (s, 1 H), 7.96 (brs, 2 H), 3.98 (s, 3 H) 4-55 CF₃ H Br 10.43 (brs), 7.96 (s, 1 H), 7.87 (d, 1 H), 7.66 (d, 1 H), 4.10 (s, 3 H) 4-56 CF₃ H SO₂Me 4-57 CF₃ H CF₃ 8.30 (brd, 1 H), 8.27 (s, 1 H), 8.18 (m, 1 H), 4.00 (s, 3 H) 4-58 NO₂ NH₂ F 4-59 NO₂ NHMe F 4-60 NO₂ NMe₂ F 4-61 NO₂ Me Cl 4-62 NO₂ NH₂ Cl 4-63 NO₂ NHMe Cl 4-64 NO₂ NH₂ Cl 2.77 (s, 6 H), 3.89 (s, 3 H), 7.39 (d, 1 H), 7.95 (s, br, 1 H) 4-65 NO₂ NH₂ Br 4-66 NO₂ NHMe Br 2.92 (d, 3 H), 4.11 (s, 3 H), 7.06 (s, br, 1 H), 7.68 (d, 1 H), 8.51 (d, 1 H 4-67 NO₂ NMe₂ Br 4-68 NO₂ NH₂ CF₃ 4.15 (s, 3 H), 6.4 (s, 2 H), 7.45 (d, 1 H), 7.7 (d, 1 H) 4-69 NO₂ NMe₂ CF₃ 4-70 NO₂ NH₂ SO₂Me 4-71 NO₂ NH₂ SO₂Et 4-72 NO₂ NHMe SO₂Me 4-73 NO₂ NMe₂ SO₂Me 4-74 NO₂ NMe₂ SO₂Et 4-75 NO₂ NH₂ 1H-1,2,4-triazol- 1-yl 4-76 NO₂ NHMe 1H-1,2,4-triazol- 1-yl 4-77 NO₂ NMe₂ 1H-1,2,4-triazol- 1-yl 4-78 Me SMe H 7.42-7.36 (m, 3 H), 3.98 (s, 3 H), 2.34 (s, 3 H) 4-79 Me SOMe H 8.10 (d, 1 H), 7.77 (d, 1 H), 7.60 (t, 1 H), 4.11 (s, 3 H), 2.70 (s, 3 H), 2.47 (s, 3 H) 4-80 Me SO₂Me H 8.11 (d, 1 H), 7.94 (d, 1 H), 7.63 (t, 1 H), 4.01 (s, 3 H), 3.28 (s, 3 H), 2.73 (s, 3 H) 4-81 Me SEt H 4-82 Me SOEt H 4-83 Me SO₂Et H 4-84 Me S(CH₂)₂OMe H 4-85 Me SO(CH₂)₂OMe H 4-86 Me SO₂(CH₂)₂OMe H 4-87 Me F F 11.63 (brs, 1 H), 7.59 (ddd, 1 H), 7.47 (m, 1 H), 3.97 (s, 3 H), 2.39 (d, 3 H) 4-88 Me SEt F 4-89 Me SOEt F 4-90 Me SO₂Et F 4-91 Me Me Cl 4-92 Me F Cl 11.69 (brs, 1 H), 7.63 (t, 1 H), 7.55 (d, 1 H), 3.98 (s, 3 H), 2.38 (d, 3 H) 4-93 Me Cl Cl 4-94 Me NH₂ Cl 4-95 Me NHMe Cl 4-96 Me NMe₂ Cl 8.94 (brs), 7.38 (d, 1 H), 7.32 (d, 1 H), 4.10 (s, 3 H), 2.87 (s, 6 H), 2.48 (s, 3 H) 4-97 Me O(CH₂)₂OMe Cl 7.51 (d, 1 H), 7.43 (d, 1 H), 6.62 (brs), 4.05 (m, 2 H), 3.97 (s, 3 H), 3.68 (m, 2 H), 3.34 (s, 3 H), 2.38 (s, 3 H) 4-98 Me O(CH₂)₃OMe Cl 11.55 (s, 1 H), 7.50 (d, 1 H), 7.43 (d, 1 H), 3.97 (s, 3 H), 3.95 (t, 2 H), 3.56 (t, 2 H), 3.26 (s, 3 H), 2.36 (s, 3 H), 2.01 (quin, 2 H) 4-99 Me O(CH₂)₄OMe Cl 4-100 Me OCH₂CONMe₂ Cl 4-101 Me O(CH₂)₂CONMe₂ Cl 11.71 (bs, 1 H), 7.50 (d, 1 H), 7.97 (d, 1 H), 4.65 (s, 2 H), 3.97 (s, 3 H), 2.98 (s, 3 H), 2.88 (s, 3 H), 2.37 (s, 3 H) 4-102 Me O(CH₂)₂—NH(CO)NMe₂ Cl 4-103 Me O(CH₂)NH(CO)NHCO₂Et Cl 4-104 Me O(CH₂)₂NHCO₂Me Cl 4-105 Me OCH₂NHSO₂cPr Cl 4-106 Me O(CH₂)-5-(2,4- Cl dimethyl-2,4- dihydro-3H-1,2,4- triazol-3-one 4-107 Me O(CH₂)-3,5-dimethyl- Cl 1,2-oxazol-4-yl 4-108 Me SMe Cl 7.59 (d, 1 H), 7.49 (d, 1 H), 4.11 (s, 3 H), 2.79 (s, 3 H), 2.38 (s, 3 H) 4-109 Me SOMe Cl 7.75 (d, 1 H), 7.58 (d, 1 H), 4.00 (s, 3 H), 3.04 (s, 3 H), 2.73 (s, 3 H) in DMSO-d₆ 4-110 Me SO₂Me Cl 7.68 (d, 1 H), 7.58 (d, 1 H), 4.14 (s, 3 H), 3.36 (s, 3 H), 2.86 (s, 3 H) 4-111 Me SEt Cl 7.36 (d, 1 H), 7.50 (d, 1 H), 4.10 (s, 3 H), 2.88 (q, 2 H), 2.79 (s, 3 H), 1.22 (t, 3 H) 4-112 Me SOEt Cl 7.63 (d, 1 H), 7.40 (d, 1 H), 4.09 (s, 3 H), 3.32 (m, 1 H), 3.11 (m, 1 H), 2.73 (s, 3 H), 1.36 (t, 3 H) 4-13 Me SO₂Et Cl 7.69 (d, 1 H), 7.57 (d, 1 H), 4.13 (s, 3 H), 3.48 (q, 2 H), 2.85 (s, 3 H), 1.38 (t, 3 H) 4-114 Me S(CH₂)₂OMe Cl 4-115 Me SO(CH₂)₂OMe Cl 4-116 Me SO₂(CH₂)₂OMe Cl 4-117 Me NH₂ Br 4-118 Me NHMe Br 4-119 Me NMe₂ Br 9.20 (brs), 7.54 (d, 1 H), 7.30 (d, 1 H), 4.10 (s, 3 H), 2.88 (s, 6 H), 2.49 (s, 3 H) 4-120 Me OCH₂CONEt₂ Br 11.60 (bs, 1 H), 7.65 (d, 1 H), 7.40 (d, 1 H), 4.59 (s, 2 H), 3.97 (s, 3 H), 3.32-3.38 (m, 4 H), 2.39 (s, 3 H), 1.14 (t, 3 H), 1.07 (t, 3 H) 4-121 Me O(CH₂)-5-pyrrolidin- Br 2-one 4-122 Me SMe Br 10.29 (bs, 1 H), 7.71 (d, 1 H), 7.53 (d, 1 H), 4.11 (s, 3 H), 2.83 (s, 3 H), 2.38 (s, 3 H) 4-123 Me SOMe Br 9.95 (bs, 1 H), 7.60 (d, 1 H), 7.51 (d, 1 H), 4.12 (s, 3 H), 2.99 (s, 3 H), 2.86 (s, 3 H) 4-124 Me SO₂Me Br 11.80 (bs, 1 H), 7.93 (d, 1 H), 7.74 (d, 1 H), 4.00 (s, 3 H), 3.45 (s, 3 H), 2.73 (s, 3 H) 4-125 Me SEt Br 10.01 (bs, 1 H), 7.70 (d, 1 H), 7.51 (d, 1 H), 4.11 (s, 3 H), 2.88 (q, 2 H), 2.81 (s, 3 H), 1.23 (t, 3 H) 4-126 Me SOEt Br 7.74 (d, 1 H), 7.64 (d, 1 H), 4.08 (s, 3 H), 3.43-3.48 (m, 1 H), 3.23-3.29 (m, 1 H); 2.82 (s, 3 H), 1.42 (t, 3 H) 4-127 Me SO₂Et Br 11.77 (bs, 1 H), 7.95 (d, 1 H), 7.76 (d, 1 H), 4.01 (s, 3 H), 3.57 (q, 2 H), 2.73 (s, 3 H), 1.25 (t, 3 H) 4-128 Me SMe I 11.60 (bs, 1 H), 8.00 (d, 1 H), 7.34 (d, 1 H), 3.98 (s, 3 H), 2.72 (s, 3 H), 2.32 (s, 3 H) 4-129 Me SOMe I 11.68 (bs, 1 H), 7.98 (d, 1 H), 7.43 (d, 1 H), 3.99 (s, 3 H), 2.96 (s, 3 H), 2.67 (s, 3 H) 4-130 Me SO₂Me I 9.42 (bs, 1 H), 8.25 (d, 1 H), 7.32 (d, 1 H), 4.13 (s, 3 H), 3.30 (s, 3 H), 2.88 (s, 3 H) 4-131 Me SEt I 9.88 (bs, 1 H), 7.99 (d, 1 H), 7.31 (d, 1 H), 4.11 (s, 3 H), 2.86 (q, 2 H), 2.85 (s, 3 H), 1.26 (t, 3 H) 4-132 Me SOEt I 8.03 (d, 1 H), 7.43 (d, 1 H), 4.08 (s, H), 3.35-3.42 (m, 1 H), 3.19- 3.24 (m, 1 H), 2.81 (s, 3 H), 1.45 (t, 3 H) 4-133 Me SO₂Et I 11.74 (bs, 1 H), 8.29 (d, 1 H), 7.50 (d, 1 H), 4.00 (s, 3 H), 3.53 (q, 2 H), 2.73 (s, 3 H), 1.26 (t, 3 H) 4-134 Me Cl CF₃ 7.89 (d, 1 H), 7.80 (d, 1 H), 4.01 (s, 3 H), 2.50 (s, 3 H) 4-135 Me SMe CF₃ 7.74 (s, 2 H), 4.14 (s, 3 H), 2.83 (s, 3 H), 2.32 (s, 3 H) 4-136 Me SOMe CF₃ 7.73 (d, 1 H), 7.67 (d, 1 H), 4.14 (s, 3 H), 3.01 (s, 3 H), 2.98 (s, 3 H) 4-137 Me SO₂Me CF₃ 8.10 (d, 1 H), 8.06 (d, 1 H), 4.03 (s, 3 H), 3.44 (s, 3 H), 2.76 (s, 3 H) 4-138 Me SEt CF₃ 7.78 (d, 1 H), 7.75 (d, 1 H), 4.13 (s, 3 H), 2.82 (s, 3 H), 2.79 (q, 2 H), 1.23 (t, 3 H) 4-139 Me SOEt CF₃ 7.77 (d, 1 H), 7.72 (d, 1 H), 4.14 (s, 3 H), 3.44 (m, 1 H), 3.00- 2.86 (m, 1 H), 2.91 (s, 3 H), 1.41 (t, 3 H) 4-140 Me SO₂Et CF₃ 7.94 (d, 1 H), 7.89 (d, 1 H), 4.14 (s, 3 H), 3.36 (q, 2 H), 2.85 (s, 3 H), 1.50 (t, 3 H) 4-141 Me S(CH₂)₂OMe CF₃ 7.79 (d, 1 H), 7.75 (d, 1 H), 4.12 (s, 3 H), 3.56 (t, 2 H), 3.33 (s, 3 H), 2.95 (t, 2 H), 2.84 (s, 3 H) 4-142 Me S(O)(CH₂)₂OMe CF₃ 7.77 (d, 1 H), 7.71 (d, 1 H), 4.13 (s, 3 H), 3.91 (dt, 1 H), 3.78 (dt, 1 H), 3.56 (dt, 1 H), 3.37 (s, 3 H), 3.09 (m, 1 H), 2.87 (s, 3 H) 4-143 Me SO₂(CH₂)₂OMe CF₃ 7.89 (d, 1 H), 7.88 (d, 1 H), 4.13 (s, 3 H), 3.92 (t, 2 H), 3.58 (t, 2 H), 3.27 (s, 3 H), 2.82 (s, 3 H) 4-144 Me 4,5-dihydro-1,2- SO₂Me 8.16 (d, 1 H), 7.96 (d, 1 H), 4.61 oxazol-3-yl (t, 2 H), 4.1 (s, 3 H), 3.39 (m, 2 H), 3.25 (s, 3 H), 2.50 (s, 3 H) 4-145 Me 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 4-146 Me 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol-3- yl 4-147 Me 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol-3- yl 4-148 Me NH₂ SO₂Me 11.61 (brs), 7.59 (d, 1 H), 6.95 (d, 1 H), 6.09 (brs, 2 H), 3.99 (s, 3 H), 3.17 (s, 3 H), 2.21 (s, 3 H) 4-149 Me NHMe SO₂Me 2.35 (s, 3 H), 2.9 (d, 3 H), 3.28 (s, 3 H), 4.0 (s, 3 H), 5.38 (q, 1 H), 7.28 (d, 1 H), 7.72 (d, 1 H) 4-150 Me NMe₂ SO₂Me 9.65 (brs), 7.99 (d, 1 H), 7.61 (d, 1 H), 4.12 (s, 3 H), 3.27 (s, 3 H), 2.91 (s, 6 H), 2.50 (s, 3 H) 4-151 Me NH(CH₂)₂OMe SO₂Me 2.43 (s, 3 H), 3.18 (s, 3 H), 3.38 (s, 3 H), 3.4 (m, 2 H), 3.6 (m, 2 H), 4.11 (s, 3 H), 7.35 (d, 1 H), 7.76 (d, 1 H) 4-152 Me pyrazol-1-yl SO₂Me 8.11 (d, 1 H), 8.07 (d, 1 H), 7.99 (d, 1 H), 7.86 (d, 1 H), 6.59 (dd, 1 H), 4.01 (s, 3 H), 3.04 (s, 3 H), 1.92 (s, 3 H) 4-153 Me OH SO₂Me 4-154 Me OMe SO₂Me 11.80 (bs, 1 H), 7.81 (d, 1 H), 7.63 (d, 1 H), 4.00 (s, 3 H), 3.90 (s, 3 H), 3.33 (s, 3 H), 2.41 (s, 3 H) 4-155 Me OMe SO₂Et 4-156 Me OEt SO₂Me 4-157 Me OEt SO₂Et 4-158 Me OiPr SO₂Me 4-159 Me OiPr SO₂Et 4-160 Me O(CH₂)₂OMe SO₂Me 7.90 (d, 1 H), 7.61 (d, 1 H), 5.20 (brs), 4.22 (m, 2 H), 4.07 (s, 3 H), 3.82 (m, 2 H), 3.48 (s, 3 H), 3.29 (s, 3 H), 2.51 (s, 3 H) 4-161 Me O(CH₂)₂OMe SO₂Et 10.50 (bs, 1 H), 7.95 (d, 1 H), 7.64 (d, 1 H), 4.24-4.26 (m, 2 H), 4.12 (s, 3 H), 3.81-3.83 (m, 2 H), 3.49 (q, 2 H), 3.47 (s, 3 H), 2.54 (s, 3 H), 1.24 (t, 3 H) 4-162 Me O(CH₂)₃OMe SO₂Me 10.00 (bs, 1 H), 7.97 (d, 1 H), 7.62 (d, 1 H), 4.18 (t, 2 H), 4.12 (s, 3 H), 3.62 (t, 2 H), 3.38 (s, 3 H), 3.27 (s, 3 H), 2.50 (s, 3 H), 2.15 (quin, 2 H) 4-163 Me O(CH₂)₃OMe SO₂Et 4-164 Me O(CH₂)₄OMe SO₂Me 4-165 Me O(CH₂)₄OMe SO₂Et 4-166 Me O(CH₂)₂NHSO2Me SO₂Me 4-167 Me O(CH₂)₂NHSO2Me SO₂Et 4-168 Me OCH₂(CO)NMe₂ SO₂Me 11.73 (bs, 1 H), 7.83 (d, 1 H), 7.67 (d, 1 H), 4.74 (s, 2 H), 4.00 (s, 3 H), 3.45 (s, 3 H), 2.90 (s, 3 H), 2.89 (s, 3 H), 2.33 (s, 3 H) 4-169 Me OCH₂(CO)NMe₂ SO₂Et 4-170 Me [1,4]dioxan-2- SO₂Me 11.73 (bs, 1 H), 7.82 (d, 1 H), ylmethoxy 7.65 (d, 1 H), 4.00-4.10 (m, 1 H), 3.99 (s, 3 H), 3.95-4.02 (m, 1 H), 3.80-3.89 (m, 2 H), 3.63- 3.72 (m, 2 H), 3.45-3.58 (m, 2 H), 3.35 (s, 3 H), 2.41 (s, 3 H) 4-171 Me [1,4]dioxan-2- SO₂Et ylmethoxy 4-172 Me O(CH₂)₂-O(3,5- SO₂Me dimethoxypyrimidin-2- yl) 4-173 Me Cl SO₂Me 8.18 (d, 1 H), 7.71 (d, 1 H), 4.14 (s, 3 H), 3.33 (s, 3 H), 2.63 (s, 3 H) 4-174 Me SMe SO₂Me 8.16 (d, 1 H), 7.79 (d, 1 H), 4.14 (s, 3 H), 3.48 (s, 3 H), 2.83 (s, 3 H), 2.43 (s, 3 H) 4-175 Me SOMe SO₂Me 8.00 (s, 2 H), 4.02 (s, 3 H), 3.49 (s, 3 H), 3.11 (s, 3 H), 2.87 (s, 3 H) 4-176 Me SO₂Me SO₂Me 8.38 (d, 1 H), 7.93 (d, 1 H), 4.14 (s, 3 H), 3.59 (s, 3 H), 3.50 (s, 3 H), 2.87 (s, 3 H) 4-177 Me SO₂Me SO₂Et 4-178 Me SEt SO₂Me 8.18 (d, 1 H), 7.78 (d, 1 H), 4.14 (s, 3 H), 3.48 (s, 3 H), 2.94 (q, 2 H), 2.81 (s, 3 H), 1.30 (t, 3 H) 4-179 Me SOEt SO₂Me 8.14 (d, 1 H), 7.84 (d, 1 H), 4.15 (s, 3 H), 3.55-3.43 (m, 1 H), 3.38 (s, 3 H), 3.35-3.23 (m, 1 H), 2.92 (s, 3 H), 1.54 (t, 3 H) 4-180 Me SO₂Et SO₂Me 8.29 (d, 1 H), 8.13 (d, 1 H), 4.01 (s, 3 H), 3.73 (q, 2 H), 3.60 (s, 3 H), 2.73 (s, 3 H), 1.38 (t, 3 H) 4-181 Me S(CH₂)₂OMe SO₂Me 8.12 (d, 1 H), 7.80 (d, 1 H), 4.13 (s, 3 H), 3.61 (t, 2 H), 3.49 (s, 3 H), 3.34 (s, 3 H), 3.10 (t, 2 H), 2.81 (s, 3 H) 4-182 Me SO(CH₂)₂OMe SO₂Me 8.14 (d, 1 H), 7.84 (d, 1 H), 4.14 (s, 3 H), 4.07-3.98 (m, 1 H), 3.92- 3.85 (m, 1 H), 3.75-3.57 (m, 1 H), 3.57-3.45 (m, 1 H), 3.44 (s, 3 H), 3.39 (s, 3 H), 2.90 (s, 3 H) 4-183 Me SO₂(CH₂)₂OMe SO₂Me 8.36 (d, 1 H), 7.92 (d, 1 H), 4.15 (s, 3 H), 4.00 (t, 2 H), 3.94 (t, 2 H), 3.56 (s, 3 H), 3.35 (s, 3 H), 2.85 (s, 3 H) 4-184 CH₂SMe OMe SO₂Me 4-185 CH₂OMe OMe SO₂Me 4-186 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 4-187 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 4-188 CH₂O(CH₂)₃OMe OMe SO₂Me 4-189 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 4-190 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 4-191 Et SMe Cl 1.22 (t, 3 H), 2.40 (s, 3 H), 3.18 (q, 2 H), 4.10 (s, 3 H), 7.48 (s, 1 H), 7.60 (s, 1 H) 4-192 Et SO₂Me Cl 1.37 (t, 3 H), 3.20 (q, 2 H), 3.30 (s, 3 H), 4.09 (s, 3 H), 7.48 (d, 1 H), 7.62 (d, 1 H) 4-193 Et SMe CF₃ 1.26 (t, 3 H), 2.36 (s, 3 H), 3.26 (q, 2 H), 4.13 (s, 3 H), 7.76 (s, 2 H), 10.79 (s, 1 H) 4-194 Et SO₂Me CF₃ 1.32 (t, 3 H), 3.30 (s, 3 H), 3.35 (q, 2 H), 4.15 (s, 3 H), 7.89 (d, 1 H), 7.91 (d, 1 H), 11.10 (br, s, 1 H) 4-195 Et F SO₂Me 11.90 (brs, 1 H), 7.87 (t, 1 H), 7.76 (t, 1 H), 4.01 (s, 3 H), 3.41 (s, 3 H), 2.82 (q, 2 H), 1.21 (t, 3 H) 4-196 Et NH(CH₂)₂OMe SO₂Me 4-197 iPr SMe CF₃ 4-198 iPr SO₂Me CF₃ 1.41 (d, 6 H), 3.32 (s, 3 H), 4.15 (s, 3 H), 4.19 (m, 1 H), 7.78 (d, 1 H), 7.85 (d, 1 H), 10.4 (br, s, 1 H) 4-199 cPr SO₂Me CF₃ 4-200 CF₃ O(CH₂)₂OMe F 4-201 CF₃ O(CH₂)₃OMe F 4-202 CF₃ OCH₂CONMe₂ F 4-203 CF₃ [1,4]dioxan-2- F ylmethoxy 4-204 CF₃ O(CH₂)₂OMe Cl 4-205 CF₃ O(CH₂)₃OMe Cl 4-206 CF₃ OCH₂CONMe₂ Cl 4-207 CF₃ [1,4]dioxan-2- Cl ylmethoxy 4-208 CF₃ O(CH₂)₂OMe Br 4-209 CF₃ O(CH₂)₂OMe Br 4-210 CF₃ O(CH₂)₃OMe Br 4-211 CF₃ OCH₂CONMe₂ Br 4-212 CF₃ [1,4]dioxan-2- Br ylmethoxy 4-213 CF₃ O(CH₂)₂OMe I 4-214 CF₃ O(CH₂)₃OMe I 4-215 CF₃ OCH₂CONMe₂ I 4-216 CF₃ [1,4]dioxan-2- I ylmethoxy 4-217 CF₃ F SO₂Me 8.19 (pt, 1 H), 7.66 (d, 1 H), 3.90 (s, 3 H), 3.25 (s, 3 H) 4-218 CF₃ F SO₂Et 8.14 (pt, 1 H), 7.66 (d, 1 H), 3.89 (s, 3 H), 3.29 (q, 2 H), 1.12 (t, 3 H) 4-219 CF₃ O(CH₂)₂OMe SO₂Me 8.31 (d, 1 H), 7.88 (d, 1 H), 4.35 (t, 2 H), 4.00 (s, 3 H), 3.76 (t, 2 H), 3.47 (s, 3 H), 3.36 (s, 3 H) 4-220 CF₃ O(CH₂)₂OMe SO₂Et 12.05 (s, 1 H), 8.30 (d, 1 H), 7.89 (d, 1 H), 4.34 (t, 2 H), 4.00 (s, 3 H), 3.75 (t, 2 H), 3.61 (q, 2 H), 3.36 (s, 3 H), 1.15 (t, 3 H) 4-221 CF₃ O(CH₂)₃OMe SO₂Me 12.04 (s, 1 H), 8.30 (d, 1 H), 7.86 (d, 1 H), 4.27 (t, 2 H), 3.97 (s, 3 H), 3.52 (t, 2 H), 3.42 (s, 3 H), 3.27 (s, 3 H), 2.08 (quin, 2 H) 4-222 CF₃ O(CH₂)₂OMe SO₂Et 12.01 (s, 1 H), 8.28 (d, 1 H), 7.86 (bs, 1 H), 4.25 (t, 2 H), 4.00 (s, 3 H), 3.49-3.56 (m, 4 H), 3.27 (s, 3 H), 2.06 (quin, 2 H), 1.12 (t, 3 H) 4-223 CF₃ OCH₂CONMe₂ SO₂Me 8.26 (s, 1 H), 7.70 (d, 1 H), 4.89 (s, 2 H), 3.95 (s, 3 H), 3.33 (s, 3 H), 2.92 (s, 3 H), 2.84 (s, 3 H) 4-224 CF₃ OCH₂CONMe₂ SO₂Et 12.05 (bs, H), 8.30 (d, 1 H), 7.92 (d, 1 H), 4.87 (s, 2 H), 4.00 (s, 3 H), 3.75 (q, 2 H), 2.88 (s, 3 H), 2.84 (s, 3 H), 1.11 (t, 3 H) 4-225 CF₃ [1,4]dioxan-2- SO₂Me ylmethoxy 4-226 CF₃ [1,4]dioxan-2- SO₂Et ylmethoxy 4-227 F SMe CF₃ 10.27 (brs, 1 H), 8.09 (t, 1 H), 7.69 (d, 1 H), 4.09 (s, 3 H), 2.54 (s, 3 H) 4-228 F SOMe CF₃ 4-229 Cl SMe H 7.50 (d, 1 H), 7.41 (t, 1 H), 7.35 (d, 1 H), 4.13 (s, 3 H), 2.53 (s, 3 H) 4-230 Cl SOMe H 8.03 (d, 1 H), 7.84 (d, 1 H), 7.68 (t, 1 H), 4.12 (s, 3 H), 2.84 (s, 3 H) 4-231 Cl SO₂Me H 4-232 Cl SEt H 4-233 Cl SOEt H 4-234 Cl SO₂Et H 4-235 Cl S(CH₂)₂OMe H 4-236 Cl SO(CH₂)₂OMe H 4-237 Cl SO₂(CH₂)₂OMe H 4-238 Cl Me Cl 7.63 (d, 1 H), 7.59 (d, 1 H), 4.00 (s, 3 H), 2.51 (s, 3 H) 4-239 Cl Cl Cl 7.85 (d, 1 H), 7.77 (d, 1 H), 4.00 (s, 3 H) 4-240 Cl OCH₂CHCH₂ Cl 4-241 Cl OCH₂CHF₂ Cl 4-242 Cl O(CH₂)₂OMe Cl 10.80 (bs, 1 H), 7.45-7.50 (m, 2 H), 4.25-4.28 (m, 2 H), 4.11 (s, 3 H), 3.81-3.84 (m, 2 H), 3.47 (s, 3 H) 4-243 Cl OCH₂(CO)NMe₂ Cl 4-244 Cl O(CH₂)-5-pyrrolidin- Cl 2-one 4-245 Cl SMe Cl 4-246 Cl SOMe Cl 4-247 Cl SO₂Me Cl 4-248 Cl F SMe 4-249 Cl Cl SO₂Me 12.06 (brs, 1 H), 8.17 (d, 1 H), 8.01 (d, 1 H), 4.02 (s, 3 H), 3.49 (s, 3 H) 4-250 Cl COOMe SO₂Me 7.98 (d, 1 H), 7.90 (d, 1 H), 3.90 (s, 3 H), 3.80 (s, 3 H), 3.27 (s, 3 H) 4-251 Cl CONMe₂ SO₂Me 8.10 (d, 1 H), 8.06 (d, 1 H), 4.02 (s, 3 H), 3.31 (s, 3 H), 3.02 (s, 3 H), 2.78 (s, 3 H) 4-252 Cl CONMe(OMe) SO₂Me 4-253 Cl CH₂OMe SO₂Me 3.25 (s, 3 H), 3.52 (s, 3 H), 4.12 (s, 3 H), 5.08 (s, 2 H), 7.78 (d, 1 H), 8.15 (d, 1 H) 4-254 Cl CH₂OMe SO₂Et 4-255 Cl CH₂OEt SO₂Me 1.25 (t, 3 H), 3.28 (s, 3 H), 3.72 (q, 2 H), 4.15 (s, 3 H), 5.15 (s, 2 H), 7.78 (d, 1 H), 8.15 (d, 1 H) 4-256 Cl CH₂OEt SO₂Et 4-257 Cl CH₂OiPr SO₂Me 4-258 Cl CH₂Ocpentyl SO₂Me 1.5-1.85 (m, 8 H), 3.3 (s, 3 H), 4.15 (s, 3 H), 4.15 (m, 1 H), 5.1 (s, 2 H), 7.78 (d, 1 H), 8.15 (d, 1 H) 4-259 Cl CH₂OCH₂CHF₂ SO₂Me 3.25 (s, 3 H), 3.88 (m, 2 H), 4.12 (s, 3 H), 5.3 (s, 2 H), 5.95 (m, 1 H), 7.75 (d, 1 H), 8.25 (d, 1 H) 4-260 Cl CH₂OCH₂CF₃ SO₂Me 8.24 (d, 1 H), 7.86 (d, 1 H), 5.39 (s, 2 H), 4.16 (s, 3 H), 4.06 (q, 2 H), 3.25 (s, 3 H) 4-261 Cl CH₂OCH₂CF₃ SO₂Et 4-262 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 3.25 (s, 3 H), 3.98 (t, 2 H), 4.15 (s, 3 H), 5.28 (s, 2 H), 6.88 (m, 1 H), 7.78 (d, 1 H), 8.25 (d, 1 H) 4-263 Cl CH₂PO₃Me₂ SO₂Me 4-264 Cl 4,5-dihydro-1,2- SMe 9.41 (brs), 7.84 (d, 1 H), 7.28 oxazol-3-yl (d, 1 H), 4.61 (t, 2 H), 4.10 (s, 3 H), 3.32 (t, 2 H), 2.53 (s, 3 H) 4-265 Cl 4,5-dihydro-1,2- SO₂Me 8.23 (d, 1 H), 7.96 (d, 1 H), 4.64 oxazol-3-yl (t, 2 H), 4.13 (s, 3 H), 3.46 (t, 2 H), 3.27 (s, 3 H) 4-266 Cl 4,5-dihydro-1,2- SO₂Et 8.17 (d, 1 H), 7.95 (d, 1 H), 4.63 oxazol-3-yl (t, 2 H), 4.15 (s, 3 H), 3.46 (t, 2 H), 3.41 (q, 2 H), 1.30 (t, 3 H) 4-267 Cl 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol-3- yl 4-268 Cl 5-cyanomethyl-4,5- SO₂Et 8.17 (d, 1 H), 7.97 (d, 1 H), 5.19 dihydro-1,2-oxazol-3- (m, 1 H), 4.14 (s, 3 H), 3.6 yl (dd, 1 H), 3.39 (q, 2 H), 3.30 (dd, 1 H), 2.92 (dd, 1 H), 2.87 (dd, 1 H), 1.32 (t, 3 H) 4-269 Cl CH₂O-tetrahydro- SO₂Me 2.02 (m, 2 H), 3.3 (s, 3 H), 3.7 furan-3-yl (m, 2 H), 3.78 (m, 2 H), 4.15 (s, 3 H), 4.38 (m, 1 H), 5.16 (s, 2 H), 7.80 (d, 1 H), 8.18 (d, 1 H) 4-270 Cl CH₂O- SO₂Et tetrahydrofuran-3-yl 4-271 Cl CH₂OCH₂- SO₂Me 8.13 (d, 1 H), 7.77 (d, 1 H), 5.18 tetrahydrofuran-2-yl (s, 2 H), 4.12 (s, 3 H), 4.08 (m, 1 H), 3.82-3.58 (m, 4 H), 3.31 (s, 3 H), 1.5-1.7 (m, 2 H), 2.01-1.81 (m, 2 H). 4-272 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-2-yl 4-273 Cl CH₂OCH₂- SO₂Me 1.5-1.7 (m, 2 H), 1.8-2.0 (m, tetrahydrofuran-3-yl 2 H), 3.3 (s, 3 H), 3.6-3.85 (m, 4 H), 4.05 (m, 1 H), 4.12 (s, 3 H), 5.18 (m, 2 H), 7.78 (d, 1 H), 8.18 (d, 1 H) 4-274 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-3-yl 4-275 Cl pyrazol-1-yl SO₂Me 4-276 Cl OMe SO₂Me 8.01 (d, 1 H), 7.62 (d, 1 H), 4.17 (s, 3 H), 4.14 (s, 3 H), 3.29 (s, 3 H) 4-277 Cl OMe SO₂Et 11.32 (bs, 1 H), 7.99 (d, 1 H), 7.60 (d, 1 H), 4.14 (s, 3 H), 4.12 (s, 3 H), 3.45 (q, 2 H), 1.28 (t, 3 H) 4-278 Cl OEt SO₂Me 10.25 (bs, 1 H), 8.04 (d, 1 H), 7.61 (d, 1 H), 4.36 (q, 2 H), 4.14 (s, 3 H), 3.31 (s, 3 H), 1.55 (t, 3 H) 4-279 Cl OEt SO₂Et 10.63 (bs, 1 H), 8.01 (d, 1 H), 7.60 (d, 1 H), 4.35 (q, 2 H), 4.14 (s, 3 H), 3.47 (q, 2 H), 1.53 (t, 3 H), 1.21 (t, 3 H) 4-280 Cl OiPr SO₂Me 10.35 (bs, 1 H), 8.08 (d, 1 H), 7.55 (d, 1 H), 5.30 (sep, 1 H), 4.15 (s, 3 H), 3.27 (s, 3 H), 1.42 (d, 6 H) 4-281 Cl OiPr SO₂Et 10.80 (bs, 1 H), 8.04 (d, 1 H), 7.53 (d, 1 H), 5.27 (quin, 1 H), 4.14 (s, 3 H), 3.44 (q, 2 H), 1.41 (d, 6 H), 1.25 (t, 3 H) 4-282 Cl O(CH₂)₂OMe SO₂Me 7.95 (d, 1 H), 7.76 (d, 1 H), 4.32 (t, 2 H), 4.01 (s, 3 H), 3.80 (t, 2 H), 3.43 (s, 3 H), 3.37 (s, 3 H) 4-283 Cl O(CH₂)₂OMe SO₂Et 11.96 (s, 1 H), 7.94 (d, 1 H), 7.77 (d, 1 H), 4.31 (t, 2 H), 4.01 (s, 3 H), 3.78 (t, 2 H), 3.54 (q, 2 H), 3.38 (s, 3 H), 1.13 (t, 3 H) 4-284 Cl O(CH₂)₃OMe SO₂Me 11.96 (s, 1 H), 7.94 (d, 1 H), 7.75 (d, 1 H), 4.25 (t, 2 H), 4.02 (s, 3 H), 3.55 (t, 2 H), 3.28 (s, 3 H), 2.11 (quin, 2 H) 4-285 Cl O(CH₂)₃OMe SO₂Et 7.93 (d, 1 H), 7.76 (d, 1 H), 4.24 (t, 2 H), 4.02 (s, 3 H), 3.54 (t, 2 H), 3.51 (q, 2 H), 3.27 (s, 3 H), 2.09 (m, 2 H), 1.13 (t, 3 H) 4-286 Cl O(CH₂)₄OMe SO₂Me 4-287 Cl O(CH₂)₄OMe SO₂Et 4-288 Cl [1,4]dioxan-2- SO₂Me 12.01 (bs, 1 H), 7.96 (d, 1 H), ylmethoxy 7.80 (d, 1 H), 4.20-4.25 (m, 1 H), 4.09-4.14 (m, 1 H), 4.01 (s, 3 H), 4.00-4.05 (m, 1 H), 3.88 (dd, 1 H), 3.80-3.83 (m, 1 H), 3.65-3.72 (m, 2 H), 3.45-3.55 (m, 2 H), 3.43 (s, 3 H) 4-289 Cl [1,4]dioxan-2- SO₂Et 10.60 (bs, 1 H), 8.03 (d, 1 H), ylmethoxy 7.63 (d, 1 H), 4.38 (dd, 1 H), 4.22 (dd, 1 H), 4.10-4.17 (m, 1 H), 4.13 (s, 3 H), 3.65-3.96 (m, 5 H), 3.59 (dd, 1 H), 3.49 (q, 2 H), 1.28 (t, 3 H) 4-290 Cl OCH₂(CO)NMe₂ SO₂Me 10.90 (bs, 1 H), 8.05 (d, 1 H), 7.67 (d, 1 H), 5.01 (s, 2 H), 4.12 (s, 3 H), 3.44 (s, 3 H), 3.04 (s, 3 H), 2.96 (s, 3 H) 4-291 Cl OCH₂(CO)NMe₂ SO₂Et 12.00 (bs, 1 H), 7.94 (d, 1 H), 7.81 (d, 1 H), 4.88 (s, 2 H), 4.02 (s, 3 H), 3.71 (q, 2 H), 2.89 (s, 3 H), 2.88 (s, 3 H), 1.11 (t, 3 H) 4-292 Cl SMe SO₂Me 11.20 (brs, 1 H), 8.20 (d, 1 H), 7.77 (d, 1 H), 4.15 (s, 3 H), 3.50 (s, 3 H), 2.54 (s, 3 H) 4-293 Cl SOMe SO₂Me 4-294 Br OMe Br 11.83 (s, 1 H), 7.85 (d, 1 H), 7.43 (d, 1 H), 4.01 (s, 3 H), 3.85 (s, 3 H) 4-295 Br O(CH₂)₂OMe Br 10.58 (brs, 1 H), 7.68 (d, 1 H), 7.33 (d, 1 H), 4.25 (m, 2 H), 4.13 (s, 3 H), 3.86 (m, 2 H), 3.48 (s, 3 H) 4-296 Br O(CH₂)₂OMe SO₂Me 4-297 Br O(CH₂)₂OMe SO₂Et 4-298 Br O(CH₂)₃OMe SO₂Me 4-299 Br O(CH₂)₃OMe SO₂Et 4-300 Br O(CH₂)₄OMe SO₂Me 4-301 Br O(CH₂)₄OMe SO₂Et 4-302 Br [1,4]dioxan-2- SO₂Me ylmethoxy 4-303 Br [1,4]dioxan-2- SO₂Et ylmethoxy 4-304 I O(CH₂)₂OMe SO₂Me 4-305 I O(CH₂)₂OMe SO₂Et 4-306 I O(CH₂)₃OMe SO₂Me 4-307 I O(CH₂)₃OMe SO₂Et 10.35 (bs, 1 H), 8.10 (d, 1 H), 7.49 (d, 1 H), 4.35 (t, 2 H), 4.21 (s, 3 H), 3.64 (t, 2 H), 3.46 (q, 2 H), 3.39 (s, 3 H), 2.23 (quin, 2 H), 1.27 (t, 3 H) 4-308 I O(CH₂)₄OMe SO₂Me 4-309 I O(CH₂)₄OMe SO₂Et 4-310 I [1,4]dioxan-2- SO₂Me ylmethoxy 4-311 I [1,4]dioxan-2- SO₂Et ylmethoxy 4-312 OMe SMe CF₃ 7.83 (d, 1 H), 7.70 (d, 1 H), 4.01 (s, 3 H), 3.96 (s, 3 H), 2.44 (s, 3 H) 4-313 OMe SOMe CF₃ 11.82 (brs, 1 H), 8.05 (d, 1 H), 7.80 (d, 1 H), 4.03 (s, 3 H), 3.98 (s, 3 H), 3.10 (s, 3 H) 4-314 OMe SO₂Me CF₃ 10.23 (brs), 8.31 (d, 1 H), 7.90 (d, 1 H), 4.19 (s, 3 H), 4.13 (s, 3 H), 3.43 (s, 3 H) 4-315 OMe SEt CF₃ 8.21 (d, 1 H), 7.68 (d, 1 H), 4.19 (s, 3 H), 4.11 (s, 3 H), 3.01 (q, 2 H), 1.22 (t, 3 H) 4-316 OMe SOEt CF₃ 4-317 OMe SO₂Et CF₃ 8.35 (d, 1 H), 7.93 (d, 1 H), 4.20 (s, 3 H), 4.14 (s, 3 H), 3.56 (q, 2 H), 1.37 (t, 3 H) 4-318 OMe S(CH₂)₂OMe CF₃ 4-319 OMe SO(CH₂)₂OMe CF₃ 4-320 OMe SO₂(CH₂)₂OMe CF₃ 4-321 OMe SMe Cl 4-322 OMe SOMe Cl 4-323 OMe SO₂Me Cl 4-324 OMe SEt Cl 4-325 OMe SOEt Cl 4-326 OMe SO₂Et Cl 4-327 OMe S(CH₂)₂OMe Cl 4-328 OMe SO(CH₂)₂OMe Cl 4-329 OMe SO₂(CH₂)₂OMe Cl 4-330 OCH₂c-Pr SMe CF₃ 8.21 (d, 1 H), 7.66 (d, 1 H), 4.25 (d, 2 H), 4.09 (s, 3 H), 2.51 (s, 3 H), 1.49 (m, 1 H), 0.72 (m, 2 H), 0.43 (m, 2 H) 4-331 OCH₂c-Pr SOMe CF₃ 8.34 (d, 1 H), 7.74 (d, 1 H), 4.54 (dd, 1 H), 4.10 (s, 3 H), 4.07 (dd, 1 H), 3.19 (s, 3 H), 1.65-1.43 (m, 1 H), 0.71-0.60 (m, 3 H), 0.44 (m, 1 H) 4-332 OCH₂c-Pr SO₂Me CF₃ 8.39 (d, 1 H), 7.91 (d, 1 H), 4.21 (d, 2 H), 4.11 (s, 3 H), 3.49 (s, 3 H), 1.67-1.43 (m, 1 H), 0.75 (m, 2 H), 0.56 (m, 2 H) 4-333 OCH₂c-Pr SEt CF₃ 4-334 OCH₂c-Pr SOEt CF₃ 4-335 OCH₂c-Pr SO₂Et CF₃ 4-336 OCH₂c-Pr S(CH₂)₂OMe CF₃ 4-337 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 4-338 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 4-339 OCH₂c-Pr SMe Cl 4-340 OCH₂c-Pr SOMe Cl 4-341 OCH₂c-Pr SO₂Me Cl 4-342 OCH₂c-Pr SEt Cl 4-343 OCH₂c-Pr SOEt Cl 4-344 OCH₂c-Pr SO₂Et Cl 4-345 OCH₂c-Pr S(CH₂)₂OMe Cl 4-346 OCH₂c-Pr SO(CH₂)₂OMe Cl 4-347 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 4-348 OCH₂c-Pr SMe SO₂Me 4-349 OCH₂c-Pr SOMe SO₂Me 4-350 OCH₂c-Pr SO₂Me SO₂Me 4-351 OCH₂c-Pr SEt SO₂Me 4-352 OCH₂c-Pr SOEt SO₂Me 4-353 OCH₂c-Pr SO₂Et SO₂Me 4-354 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 4-355 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 4-356 OCH₂c-Pr SO₂(CH₂)₂OMe SO₂Me 4-357 SO₂Me F CF₃ 4-358 SO₂Me NH₂ CF₃ 7.78 (d, 1 H), 7.00 (d, 1 H), 6.14 (brs, 2 H), 4.18 (s, 3 H), 3.30 (s, 3 H) 4-359 SO₂Me NHEt Cl 4-360 SMe SEt F 4-361 SMe SMe F 11.62 (brs, 1 H), 7.60 (t, 1 H), 7.44 (t, 1 H), 4.03 (s, 3 H), 2.54 (d, 3 H), 2.44 (s, 3 H) 4-362 Me H F 10.35 (brs, 1 H), 7.88 (dd, 1 H), 7.08-7.02 (m, 2 H), 4.08 (s, 3 H) 4-363 Me H OCF₃ 11.58 (brs, 1 H), 7.80 (d, 1 H), 7.40 (s, 1 H), 7.37 (d, 1 H), 3.98 (s, 3 H), 2.48 (s, 3 H) 4-364 Et H F 11.50 (brs, 1 H), 7.73 (dd, 1 H), 7.26 (dd, 1 H), 7.20 (ddd, 1 H), 3.97 (s, 3 H), 2.80 (q, 2 H), 1.19 (t, 3 H) 4-365 Cl H I 9.65 (brs, 1 H), 7.91 (d, 1 H), 7.80 (dd, 1 H), 7.56 (d, 1 H), 4.10 (s, 3 H) 4-366 Cl H CN 10.55 (brs, 1 H), 7.90 (d, 1 H), 7.84 (d, 1 H), 7.74 (dd, 1 H), 4.13 (s, 3 H) 4-367 Cl H NMe₂ 9.22 (brs, 1 H), 7.95 (d, 1 H), 6.6 (d, 1 H), 6.65 (dd, 1 H), 4.06 (s, 3 H), 3.08 (s, 6 H) 4-368 Cl H NHAc 11.8 (brs, 1 H), 10.3 (brs, 1 H), 7.93 (d, 1 H), 7.72 (dd, 1 H), 7.54 (d, 1 H), 3.99 (s, 3 H), 2.09 (s, 3 H) 4-369 Cl H pyrrol-1-yl 9.79 (brs, 1 H), 8.00 (d, 1 H), 7.55 (d, 1 H), 7.47 (dd, 1 H), 4.11 (s, 3 H), 3.37 (m, 4 H), 2.07 (m, 4 H) 4-370 Cl H pyrrolidin-1-yl 9.21 (brs, 1 H), 7.94 (d, 1 H), 6.54 (d, 1 H), 6.51 (dd, 1 H), 7.16 (dd, 1 H), 6.42 (dd, 1 H), 4.11 (s, 3 H) 4-371 Cl H pyrazol-1-yl 8.71 (dd, 1 H), 8.14 (dd, 1 H), 8.01 (dd, 1 H), 7.90 (d, 1 H), 7.85 (d, 1 H), 6.64 (dd, 1 H), 4.00 (s, 3 H) 4-372 Cl H 1,2,4-triazol-1-yl 8.69 (s, 1 H), 8.17 (s, 1 H), 8.05 (d, 1 H), 7.99 (d, 1 H), 7.80 (dd, 1 H), 4.13 (s, 3 H) 4-373 Cl H 4-methyl-3- 11.84 (brs, 1 H), 8.11 (d, 1 H), trifluoromethyl- 7.99 (dd, 1 H), 7.92 (d, 1 H), 4.00 1,2,4-triazolin-5- (s, 3 H), 3.38 (s, 3 H) on-1-yl 4-374 Cl H SOMe 7.95 (d, 1 H), 7.91 (d, 1 H), 7.81 (dd, 1 H), 4.01 (s, 3 H), 2.85 (s, 3 H) 4-375 Br H F 11.8 (brs, 1 H), 7.82 (dd, 1 H), 7.78 (dd, 1 H), 7.45 (ddd, 1 H), 4.01 (s, 3 H) 4-376 Br H SMe 7.62 (d, 1 H), 7.58 (d, 1 H), 7.39 (dd, 1 H), 3.99 (s, 3 H), 2.55 (s, 3 H) 4-377 NHSO₂Me H CF₃ 4-378 NHSO₂Et H CF₃ 4-379 NHSO₂CF₃ H CF₃ 4-380 NHSO₂Me H SO₂Me 4-381 NHSO₂Et H SO₂Me 4-382 NHSO₂CF₃ H SO₂Me 4-383 NMeSO₂Me H CF₃ 4-384 NMeSO₂Et H CF₃ 4-385 NMeSO₂CF₃ H CF₃ 4-386 NMeSO₂Me H SO₂Me 4-387 NMeSO₂Et H SO₂Me 4-388 NMeSO₂CF₃ H SO₂Me 4-389 OMe H SO₂Me 10.14 (brs, 1 H), 8.45 (d, 1 H), 7.72 (d, 1 H), 7.68 (s, 1 H), 4.20 (s, 3 H), 4.08 (s, 3 H), 3.13 (s, 3 H) 4-390 OSO₂Me H CF₃ 4-391 OSO₂Et H CF₃ 4-392 OSO₂CF₃ H CF₃ 4-393 OSO₂Me H SO₂Me 4-394 OSO₂Et H SO₂Me 4-395 OSO₂CF₃ H SO₂Me 4-396 SMe H CF₃ 11.02 (brs, 1 H), 8.09 (d, 1 H), 7.59 (s, 1 H), 7.58 (d, 1 H), 4.12 (s, 3 H), 2.55 (s, 3 H) 4-397 SOMe H CF₃ 8.41 (s, 1 H), 8.38 (d, 1 H), 8.20 (d, 1 H), 3.98 (s, 3 H), 2.86 (s, 3 H) 4-398 SMe H F 10.91 (brs, 1 H), 8.06 (dd, 1 H), 7.08-7.00 (m, 2 H), 4.09 (s, 3 H), 2.49 (s, 3 H) 4-399 SMe H Cl 10.75 (brs, 1 H), 7.93 (d, 1 H), 7.33 (d, 1 H), 7.30 (dd, 1 H), 4.09 (s, 3 H), 2.51 (s, 3 H) 4-400 SMe H Br 11.64 (brs, 1 H), 7.68 (d, 1 H), 7.57 (d, 1 H), 7.52 (dd, H), 3.96 (s, 3 H), 2.27 (s, 3 H) 4-401 SMe H SMe 7.72 (d, 1 H), 7.18 (s, 1 H), 7.16 (d, 1 H), 3.94 (s, 3 H), 2.57 (s, 3 H), 2.47 (s, 3 H) 4-402 SO₂Me H SO₂Me 8.50 (s, 1 H), 8.45 (d, 1 H), 8.21 (d, 1 H), 4.05 (s, 3 H), 3.45 (s, 3 H), 3.40 (s, 3 H) 4-403 SO₂NMePh H Cl 11.82 (brs, 1 H), 7.91 (d, 1 H), 7.86 (d, 1 H), 7.42-7.32 (m, 3 H), 7.24-7.20 (m, 3 H), 3.99 (s, 3 H), 3.21 (s, 3 H) 4-404 SO₂NMe₂ H CF₃ 11.87 (brs, 1 H), 8.25 (d, 1 H), 8.11 (s, 1 H), 8.12 (d, 1 H), 4.05 (s, 3 H), 2.77 (s, 6 H) 4-405 Me OMe CF₃ 10.76 (bs, 1 H), 7.64 (s, 2 H), 4.12 (s, 3 H), 3.89 (s, 3 H), 2.53 (s, 3 H) 4-406 Me SMe CN 7.78 (d, 1 H), 7.73 (d, 1 H), 4.13 (s, 3 H), 2.76 (s, 3 H), 2.53 (s, 3 H) 4-407 Me SOMe CN 4-408 Me SO₂Me CN 8.04 (d, 1 H), 8.03 (d, 1 H), 4.09 (s, 3 H), 3.38 (s, 3 H), 2.89 (s, 3 H) 4-409 Me Me Cl 9.74 (brs, 1 H), 7.47 (d, 1 H), 7.38 (d, 1 H), 4.10 (s, 3 H), 2.47 (s, 3 H), 2.41 (s, 3 H) 4-410 Me O(CH₂)₂N(Me)SO₂Me Cl 11.56 (bs, 1 H), 7.52 (d, 1 H), 7.46 (d, 1 H), 4.05 (t, 2 H), 3.98 (s, 3 H), 3.54 (t, 2 H), 2.95 (s, 3 H), 2.94 (s, 3 H), 2.40 (s, 3 H) 4-411 Me O(CH₂)₃SMe Br 11.60 (bs, 1 H), 7.65 (d, 1 H), 7.37 (d, 1 H), 3.97 (s, 3 H), 3.96 (t, 2 H), 2.72 (t, 2 H), 2.38 (s, 3 H), 2.09 (s, 3 H), 2.06 (quin, 2 H) 4-412 Me O(CH₂)₂SEt Br 11.60 (bs, 1 H), 7.66 (d, 1 H), 7.38 (d, 1 H), 4.03 (t, 2 H), 3.98 (s, 3 H), 2.97 (t, 2 H), 2.63 (q, 2 H), 2.41 (s, 3 H), 1.22 (t, 3 H) 4-413 Me O(CH₂)₂SMe Br 11.60 (bs, 1 H), 7.66 (d, 1 H), 7.38 (d, 1 H), 4.05 (t, 2 H), 3.98 (s, 3 H), 2.93 (t, 2 H), 2.42 (s, 3 H), 2.17 (s, 3 H) 4-414 Me O(CH₂)₃SMe Cl 11.61 (bs, 1 H), 7.51 (d, 1 H), 7.45 (d, 1 H), 3.97 (t, 2 H), 3.97 (s, 3 H), 2.71 (t, 2 H), 2.37 (s, 3 H), 2.09 (s, 3 H), 2.05 (quin, 2 H) 4-415 Me O(CH₂)₂SEt Cl 11.59 (bs, 1 H), 7.51 (d, 1 H), 7.46 (d, 1 H), 4.05 (t, 2 H), 3.98 (s, 3 H), 2.95 (t, 2 H), 2.63 (q, 2 H), 2.40 (s, 3 H), 1.21 (t, 3 H) 4-416 Me O(CH₂)₂SMe Cl 11.60 (bs, 1 H), 7.52 (d, 1 H), 7.46 (d, 1 H), 4.07 (t, 2 H), 3.98 (s, 3 H), 2.92 (t, 2 H), 2.41 (s, 3 H), 2.16 (s, 3 H) 4-417 Me OEt Cl 11.59 (bs, 1 H), 7.51 (d, 1 H), 7.44 (d, 1 H), 3.97 (s, 3 H), 3.97 (q, 2 H), 2.37 (s, 3 H), 1.39 (t, 3 H) 4-418 Me OMe Cl 11.65 (bs, 1 H), 7.50 (d, 1 H), 7.44 (d, 1 H), 3.97 (s, 3 H), 3.79 (s, 3 H), 2.37 (s, 3 H) 4-419 Me tetrahydrofuran-2- Cl 7.31 (s, 2 H), 4.20-4.23 (m, 1 H), ylmethoxy 3.94 (s, 3 H), 3.80-3.87 (m, 3 H), 3.71-3.76 (m, 1 H), 2.37 (s, 3 H), 1.97-2.03 (m, 1 H), 1.76-1.92 (m, 4 H) 4-420 Me 1,4-dioxan-2- Cl 11.55 (s, 1 H), 7.49 (d, 1 H), ylmethoxy 7.44 (d, 1 H), 3.97 (s, 3 H), 3.86- 3.97 (m, 3 H), 3.78-3.81 (m, 1 H), 3.62-3.69 (m, 2 H), 3.40- 3.54 (m, 3 H), 2.37 (s, 3 H) 4-421 Me O(CH₂)₂NHSO₂iPr Cl 4-422 Me O(CH₂)₂NHCOOMe Cl 11.60 (bs, 1 H), 7.50 (d, 1 H), 7.44 (d, 1 H), 3.97 (s, 3 H), 3.91 (t, 2 H), 3.55 (s, 3 H), 3.38 (t, 2 H), 2.35 (s, 3 H) 4-423 Me OMe Br 11.59 (bs, 1 H), 7.65 (d, 1 H), 7.37 (d, 1 H), 3.97 (s, 3 H), 3.77 (s, 3 H), 2.39 (s, 3 H) 4-424 Me OEt Br 11.57 (bs, 1 H), 7.64 (d, 1 H), 7.36 (d, 1 H), 3.97 (s, 3 H), 3.95 (q, 2 H), 2.38 (s, 3 H), 1.40 (t, 3 H) 4-425 Me O(CH₂)₂OMe Br 11.60 (bs, 1 H), 7.64 (d, 1 H), 7.36 (d, 1 H), 4.03 (t, 2 H), 3.97 (s, 3 H), 3.70 (t, 2 H), 3.34 (s, 3 H), 2.39 (s, 3 H) 4-426 Me O(CH₂)₃OMe Br 11.60 (bs, 1 H), 7.64 (d, 1 H), 7.36 (d, 1 H), 3.97 (s, 3 H), 3.93 (t, 2 H), 3.56 (t, 2 H), 3.28 (s, 3 H), 2.38 (s, 3 H), 2.04 (quin, 2 H) 4-427 Me tetrahydrofuran-2- Br 11.60 (bs, 1 H), 7.64 (d, 1 H), ylmethoxy 7.36 (d, 1 H), 4.21-4.24 (m, 1 H), 3.97 (s, 3 H), 3.87 (d, 2 H), 3.79-3.86 (m, 1 H), 3.69-3.74 (m, 1 H), 2.40 (s, 3 H), 1.95-2.05 (m, 1 H), 1.75-1.88 (m, 3 H) 4-428 Me 1,4-dioxan-2- Br 11.60 (bs, 1 H), 7.64 (d, 1 H), ylmethoxy 7.37 (d, 1 H), 3.97 (s, 3 H), 3.84- 3.95 (m, 4 H), 3.75-3.83 (m, 1 H), 3.60-3.70 (m, 2 H), 3.45- 3.55 (m, 2 H), 2.38 (s, 3 H) 4-429 Me SMe NMe₂ 7.71 (d, 1 H), 6.98 (d, 1 H), 4.08 (s, 3 H), 2.92 (s, 6 H), 2.75 (s, 3 H), 2.29 (s, 3 H) 4-430 Me SOMe NMe₂ 4-431 Me SO₂Me NMe₂ 4-432 Me SMe imidazol-1-yl 7.66 (d, 1 H), 7.21 (s, 2 H), 7.05 (s, 1 H), 4.17 (s, 3 H), 2.75 (s, 3 H), 1.95 (s, 3 H) 4-433 Me SMe 1,2,4-triazol-1-yl 8.64 (s, 1 H), 8.15 (s, 1 H), 7.74 (d, 1 H), 7.53 (d, 1 H), 4.15 (s, 3 H), 2.82 (s, 3 H), 2.06 (s, 3 H) 4-434 Me SO₂Me imidazol-1-yl 9.03 (s, 1 H), 8.02 (d, 1 H), 7.72 (s, 1 H), 7.65 (d, 1 H), 7.59 (s, 1 H), 4.03 (s, 3 H), 3.34 (s, 3 H), 2.80 (s, 3 H) 4-435 Me SOMe 1,2,4-triazol-1-yl 8.72 (s, 1 H), 8.19 (s, 1 H), 7.87 (d, 1 H), 7.54 (d, 1 H), 4.01 (s, 3 H), 3.10 (s, 3 H), 2.66 (s, 3 H) 4-436 Me SO₂Me 1,2,4-triazol-1-yl 8.71 (s, 1 H), 8.20 (s, 1 H), 7.98 (d, 1 H), 7.58 (d, 1 H), 4.01 (s, 3 H), 3.36 (s, 3 H), 2.76 (s, 3 H) 4-437 Me SMe OMe 7.85 (d, 1 H), 6.91 (d, 1 H), 4.08 (s, 3 H), 3.99 (s, 3 H), 2.76 (s, 3 H), 2.33 (s, 3 H) 4-438 Me SOMe OMe 7.86 (d, 1 H), 7.28 (d, 1 H), 4.08 (s, 3 H), 4.07 (s, 3 H), 3.35 (s, 3 H), 2.80 (s, 3 H) 4-439 Me SO₂Me OMe 7.82 (d, 1 H), 7.26 (d, 1 H), 4.05 (s, 3 H), 4.00 (s, 3 H), 3.46 (s, 3 H), 2.71 (s, 3 H) 4-440 Me SEt OMe 7.76 (d, 1 H), 6.88 (d, 1 H), 4.09 (s, 3 H), 3.97 (s, 3 H), 2.83 (q, 2 H), 2.74 (s, 3 H), 1.17 (t, 3 H) 4-441 Me SOEt OMe 7.77 (d, 1 H), 6.82 (d, 1 H), 4.05 (s, 3 H), 3.96 (s, 3 H), 3.50- 3.40 (m, 1 H), 3.28-3.20 (m, 1 H), 2.67 (s, 3 H), 1.22 (t, 3 H) 4-442 Me SO₂Et OMe 7.80 (d, 1 H), 7.02 (d, 1 H), 4.12 (s, 3 H), 4.03 (s, 3 H), 3.43 (q, 2 H), 2.84 (s, 3 H), 1.31 (t, 3 H) 4-443 Me SMe OEt 7.80 (d, 1 H), 6.87 (d, 1 H), 4.20 (q, 2 H), 4.08 (s, 3 H), 2.74 (s, 3 H), 2.35 (s, 3 H), 1.53 (t, 3 H) 4-444 Me SOMe OEt 4-445 Me SO₂Me OEt 7.82 (d, 1 H), 7.02 (d, 1 H), 4.28 (q, 2 H), 4.11 (s, 3 H), 3.34 (s, 3 H), 2.82 (s, 3 H), 1.55 (t, 3 H) 4-446 Me Me SMe 9.81 (brs, 1 H), 7.57 (d, 1 H), 7.11 (d, 1 H), 4.09 (s, 3 H), 2.51 (s, 3 H), 2.45 (s, 3 H), 2.33 (s, 3 H) 4-447 Me Me SO₂Me 8.06 (d, 1 H), 7.59 (d, 1 H), 4.13 (s, 3 H), 3.13 (s, 3 H), 2.72 (s, 3 H), 2.47 (s, 3 H) 4-448 Me Me SEt 7.43 (d, 1 H), 7.17 (d, 1 H), 4.11 (s, 3 H), 2.99 (q, 2 H), 2.44 (s, 3 H), 2.35 (s, 3 H), 1.38 (t, 3 H) 4-449 Me Me SO₂Et 8.03 (d, 1 H), 7.58 (d, 1 H), 4.15 (s, 3 H), 3.20 (q, 2 H), 2.69 (s, 3 H), 2.47 (s, 3 H), 1.31 (t, 3 H) 4-450 Me NHiPr SO₂Me 11.70 (brs), 7.77 (d, 1 H), 7.27 (d, 1 H), 5.6 (brs, 1 H), 4.00 (s, 3 H), 3.63 (m, 1 H), 3.29 (s, 3 H), 2.32 (s, 3 H), 1.15 (d, 6 H) 4-451 Me NHCH₂- SO₂Me 7.73 (d, 1 H), 7.29 (d, 1 H), 5.73 tetrahydrofuran-2-yl (bs, 1 H), 4.15 (m, 1 H), 4.00 (s, 3 H), 3.85-3.66 (m, 4 H), 3.17 (s, 3 H), 2.34 (s, 3 H), 2.02-1.55 (m, 4 H) 4-452 Me NHCH₂CONHEt SO₂Me 8.15 (t, 1 H), 7.72 (d, 1 H), 7.27 (d, 1 H), 6.18 (t, 1 H), 3.99 (s, 3 H), 3.88 (d, 2 H), 3.32 (s, 3 H), 3.14 (m, 2 H), 2.32 (s, 3 H), 1.04 (t, 3 H) 4-453 Me NH(CH₂)₂OEt SO₂Me 1.23 (t, 3 H), 2.45 (s, 3 H), 3.20 (s, 3 H), 3.42 (m, 2 H), 3.56 (q, 2 H), 3.65 (m, 2 H), 4.11 (s, 3 H), 7.25 (d, 1 H), 7.78 (d, 1 H), 10.40 (s, 1 H) 4-454 Me NHEt SO₂Me 1.30 (t, 3 H), 2.46 (s, 3 H), 3.10 (s, 3 H), 3.27 (q, 2 H), 4.11 (s, 3 H), 5.54 (s, br, 1 H), 7.26 (d, 1 H), 7.79 (d, 1 H), 10.75 (s, 1 H) 4-455 Me NHnPr SO₂Me 1.03 (t, 3 H), 1.69 (m, 2 H), 2.46 (s, 3 H), 3.09 (s, 3 H), 3.19 (t, 2 H), 4.11 (s, 3 H), 5.66 (s, br, 1 H), 7.25 (d, 1 H), 7.79 (d, 1 H), 10.64 (s, 1 H) 4-456 Me NHCH₂iPr SO₂Me 1.05 (d, 3 H), 1.93 (m, 1 H), 2.46 (s, 3 H), 3.04 (d, 2 H), 3.09 (s, 3 H), 4.12 (s, 3 H), 5.75 (s, br, 1 H), 7.24 (d, 1 H), 7.81 (d, 1 H), 10.24 (s, 1 H) 4-457 Me NHCH₂cPr SO₂Me 0.28 (m, 2 H), 0.60 (m, 2 H), 1.11 (m, 1 H), 2.44 (s, 3 H), 3.12 (d, 2 H), 3.14 (s, 3 H), 4.12 (s, 3 H), 5.88 (s, br, 1 H), 7.22 (d, 1 H), 7.82 (d, 1 H), 9.91 (s, 1 H) 4-458 Me NHCH₂CH(OMe)CH₂OMe SO₂Me 2.46 (s, 3 H), 3.18 (s, 3 H), 3.23 (m, 1 H), 3.39 (s, 3 H), 3.48 (s, 3 H), 3.48 (m, 1 H), 3.55 (m, 2 H), 3.58 (m, 1 H), 4.11 (s, 3 H), 5.84 (s, br, 1 H), 7.27 (d, 1 H), 7.78 (d, 1 H), 10.46 (s, 1 H) 4-459 Me NHCH₂CH₂CH₂OCOMe SO₂Me 2.00 (m, 2 H), 2.07 (s, 3 H), 2.45 (s, 3 H), 3.11 (s, 3 H), 3.29 (t, 2 H), 4.10 (s, 3 H), 4.21 (t, 2 H), 7.30 (d, 1 H), 7.76 (d, 1 H), 11.2 (s, br, 1 H) 4-460 Me NHCH₂CH₂(1,3- SO₂Me 1.38 (dd, 1 H), 1.98 (m, 2 H), 2.12 dioxan-2-yl) (m, 1 H), 2.45 (s, 3 H), 3.14 (s, 3 H), 3.32 (s, br, 2 H), 3.79 (m, 2 H), 4.11 (s, 3 H), 4.14 (m, 2 H), 4.77 (t, 1 H), 5.72 (s, br, 1 H), 7.27 (d, 1 H), 7.78 (d, 1 H), 10.44 (s, 1 H) 4-461 Me NHCH₂Ph SO₂Me 2.56 (s, 3 H), 2.68 (s, 3 H), 4.11 (s, 3 H), 4.41 (s, 2 H), 5.98 (s, br, 1 H), 7.32 (d, 1 H), 7.34 (m, 5 H), 7.78 (d, 1 H), 10.88 (s, 1 H) 4-462 Me N(CH₃)CH₂cPr SO₂Me 0.12 (m, 1 H), 0.22 (m, 1 H), 0.47 (m, 1 H), 0.64 (m, 1 H), 1.09 (m, 1 H), 2.44 (s, 3 H), 2.65 (m, 1 H), 2.95 (s, 3 H), 3.19 (m, 1 H), 3.34 (s, 3 H), 4.10 (s, 3 H), 7.60 (d, 1 H), 7.91 (d, 1 H) 4-463 Me NHCH(CH₃)CH₂OMe SO₂Me 1.23 (d, 3 H), 2.42 (s, 3 H), 3.18 (s, 3 H), 3.30 (s, 3 H), 3.35-3.48 (m, 2 H), 3.82 (m, 1 H), 4.12 (s, 3 H), 5.95 (d, 1 H), 7.22 (d, 1 H), 7.81 (d, 1 H), 10.04 (s, 1 H) 4-464 Me NHCH(CH₃)CH₂OEt SO₂Me 1.22 (t, 3 H), 1.92 (q, 2 H), 2.47 (s, 3 H), 3.13 (s, 3 H), 3.32 (t, 2 H), 3.51 (q, 2 H), 3.58 (t, 2 H), 4.11 (s, 3 H), 5.63 (s, br, 1 H), 7.29 (d, 1 H), 7.80 (d, 1 H), 10.73 (s, 1 H) 4-465 Me NHCH₂CH(OMe)₂ SO₂Me 2.35 (s, 3 H), 3.29 (m, 2 H), 3.30 (s, 3 H), 3.33 (s, 3 H), 3.35 (s, 3 H), 3.99 (s, 3 H), 4.57 (t, 1 H), 5.69 (t, 1 H), 7.27 (d, 1 H), 7.72 (d, 1 H), 11.6 (s, br, 1 H) 4-466 Me NHCH₂CH(Me)(OMe) SO₂Me 1.22 (d, 3 H), 2.45 (s, 3 H), 3.06 (dd, 1 H), 3.18 (s, 3 H), 3.39 (s, 3 H), 3.42 (m, 1 H), 3.60 (m, 1 H), 4.11 (s, 3 H), 5.9 (s, br, 1 H), 7.25 (d, 1 H), 7.77 (d, 1 H), 10.64 (s, 1 H) 4-467 Me NCH₂(1,3-dioxan-2-yl) SO₂Me 1.40 (d, 1 H), 2.13 (m, 1 H), 2.43 (s, 3 H), 3.39 (s, br, 2 H), 3.83 (m, 2 H), 4.11 (s, 3 H), 4.14 (m, 2 H), 4.79 (t, 1 H), 5.93 (s, br, 1 H), 7.23 (d, 1 H), 7.75 (d, 1 H), 10.13 (s, 1 H) 4-468 Me 4-Me-pyrazol-1-yl SO₂Me 4-469 Me 3,5-Me₂-pyrazol-1-yl SO₂Me 8.20 (d, 1 H), 7.98 (d, 1 H), 6.12 (s, 1 H), 4.13 (s, 3 H), 3.06 (s, 3 H), 2.32 (s, 3 H), 2.11 (s, 3 H), 2.05 (s, 3 H) 4-470 Me 4-MeO-pyrazol-1-yl SO₂Me 4-471 Me 4-CN-pyrazol-1-yl SO₂Me 8.97 (d, 1 H), 8.48 (d, 1 H), 8.15 (s, 2 H), 4.01 (s, 3 H), 3.19 (s, 3 H), 1.99 (s, 3 H) 4-472 Me 4-Cl-pyrazol-1-yl SO₂Me 4-473 Me 1,2,3-triazol-1-yl SO₂Me 8.31 (d, 1 H), 8.20 (d, 1 H), 7.99 (d, 1 H), 7.91 (d, 1 H), 4.16 (s, 3 H), 2.97 (s, 3 H), 2.01 (s, 3 H) 4-474 Me 1,2,4-triazol-1-yl SO₂Me 4-475 Me 5-iPr-1,2,4-triazol-1-yl SO₂Me 4-476 Me 5-EtS-1,2,4-triazol-1-yl SO₂Me 4-477 Me O(CH₂)₂SMe SO₂Me 11.20 (bs, 1 H), 7.96 (d, 1 H), 7.70 (d, 1 H), 4.25 (t, 2 H), 4.11 (s, 3 H), 3.31 (s, 3 H), 3.00 (t, 2 H), 2.55 (s, 3 H), 2.22 (s, 3 H) 4-478 Me O(CH₂)₃SMe SO₂Me 11.00 (bs, 1 H), 7.93 (d, 1 H), 7.66 (d, 1 H), 4.17 (t, 2 H), 4.10 (s, 3 H), 3.25 (s, 3 H), 2.74 (t, 2 H), 2.51 (s, 3 H), 2.19 (quin, 2 H), 2.15 (s, 3 H) 4-479 Me tetrahydrofuran-2- SO₂Me 7.78 (d, 1 H), 7.69 (d, 1 H), ylmethoxy 4.37-4.43 (m, 1 H), 4.00-4.12 (m, 2 H), 3.91 (s, 3 H), 3.85-4.00 (m, 2 H), 2.07-2.17 (m, 1 H), 1.93-2.05 (m, 2 H), 1.78-1.88 (m, 1 H) 4-480 Me F SMe 7.55 (d, 1 H), 7.30 (t, 1 H), 3.95 (s, 3 H), 2.53 (s, 3 H), 2.34 (d, 3 H) 4-481 Me SMe SO₂Et 4-482 Me SOMe SO₂Et 4-483 Me SEt SO₂Et 4-484 Me SOEt SO₂Et 4-485 Me SO₂Et SO₂Et 4-486 Me SCH₂CF₃ SO₂Me 8.23 (d, 1 H), 7.92 (d, 1 H), 4.10 (s, 3 H), 3.75 (q, 2 H), 3.49 (s, 3 H), 2.83 (s, 3 H) 4-487 Me SOCH₂CF₃ SO₂Me 4-488 Me SO₂CH₂CF₃ SO₂Me 4-489 Me S(CH₂)₂OMe SO₂Et 4-490 Me SO(CH₂)₂OMe SO₂Et 4-491 Me SO₂(CH₂)₂OMe SO₂Et 4-492 Me S(4-F—Ph) SO₂Me 8.30 (d, 1 H), 7.83 (d, 1 H), 7.12- 7.08 (m, 2 H), 7.00-6.96 (m, 2 H), 4.10 (s, 3 H), 3.42 (s, 3 H), 2.46 (s, 3 H) 4-493 Me SO(4-F—Ph) SO₂Me 4-494 Me SO₂(4-F—Ph) SO₂Me 8.51 (d, 1 H), 8.20 (m, 2 H), 7.99 (d, 1 H), 7.24 (t, 2 H), 4.09 (s, 3 H), 3.69 (s, 3 H), 2.57 (s, 3 H) 4-495 Et SEt Cl 7.59 (d, 1 H), 7.49 (d, 1 H), 4.11 (s, 3 H), 3.20 (q, 2 H), 2.92 (q, 2 H), 1.23 (t, 3 H), 1.21 (t, 3 H) 4-496 Et SOEt Cl 7.65 (d, 1 H), 7.39 (d, 1 H), 4.08 (s, 3 H), 3.56 (m, 1 H), 3.18 (m, 1 H), 3.12-2.96 (m, 2 H), 1.39 (t, 3 H), 1.19 (t, 3 H) 4-497 Et SO₂Et Cl 7.68 (d, 1 H), 7.57 (d, 1 H), 4.13 (s, 3 H), 3.52 (q, 2 H), 3.32 (q, 2 H), 1.38 (t, 3 H), 1.31 (t, 3 H) 4-498 Et S(CH₂)₂OMe Cl 4-499 Et SO(CH₂)₂OMe Cl 4-500 Et SO₂(CH₂)₂OMe Cl 4-501 Et SOMe Cl 1.25 (t, 3 H), 3.12 (s, 3 H), 3.12 (m, 1 H), 3.29 (m, 1 H), 4.12 (s, 3 H), 7.42 (d, 1 H), 7.62 (d, 1 H) 4-502 Et SMe Br 1.21 (t, 3 H), 2.39 (s, 3 H), 3.10 (q, 2 H), 3.97 (s, 3 H), 7.58 (d, 1 H), 7.76 (d, 1 H), 11.7 (br, s, 1 H) 4-503 Et SOMe Br 1.25 (t, 3 H), 3.10 (s, 3 H), 3.19 (m, 1 H), 3.35 (m, 1 H), 4.13 (s, 3 H), 7.55 (d, 1 H), 7.65 (d, 1 H), 4-504 Et SO₂Me Br 1.05 (t, 3 H), 3.25 (q, 2 H), 3.32 (s, 3 H), 3.89 (s, 3 H), 7.44 (d, 1 H), 7.59 (d, 1 H), 8.54 (s, 1 H) 4-505 Et SOMe CF₃ 1.26 (t, 3 H), 3.03 (s, 3 H), 3.45 (m, 1 H), 3.62 (m, 1 H), 4.11 (s, 3 H), 7.71 (d, 1 H), 7.79 (d, 1 H) 4-506 Et SEt CF₃ 4-507 Et SOEt CF₃ 4-508 Et SO₂Et CF₃ 4-509 Et S(CH₂)₂OMe CF₃ 4-510 Et SO(CH₂)₂OMe CF₃ 4-511 Et SO₂(CH₂)₂OMe CF₃ 4-512 Et NHiPr SO₂Me 1.18 (t, 3 H), 1.22 (d, 6 H), 2.89 (q, 2 H), 3.13 (s, 3 H), 3.77 (m, 1 H), 4.13 (s, 3 H), 5.58 (s, br, 1 H), 7.15 (d, 1 H), 7.83 (d, 1 H), 9.91 (s, 1 H) 4-513 Et SMe SO₂Et 4-514 Et SOMe SO₂Et 4-515 Et SO₂Me SO₂Et 4-516 Et SEt SO₂Et 4-517 Et SOEt SO₂Et 4-518 Et SO₂Et SO₂Et 4-519 Et S(CH₂)₂OMe SO₂Et 4-520 Et SO(CH₂)₂OMe SO₂Et 4-521 Et SO₂(CH₂)₂OMe SO₂Et 4-522 Et SEt SO₂Me 4-523 Et SOEt SO₂Me 4-524 Et SO₂Et SO₂Me 4-525 Et S(CH₂)₂OMe SO₂Me 4-526 Et SO(CH₂)₂OMe SO₂Me 4-527 Et SO₂(CH₂)₂OMe SO₂Me 4-528 Et SMe SO₂Me 4-529 Et SOMe SO₂Me 4-530 Et SO₂Me SO₂Me 4-531 nPr SMe Cl 0.97 (t, 3 H), 1.61 (m, 2 H), 2.41 (s, 3 H), 3.13 (m, 2 H), 4.11 (s, 3 H), 7.50 (d, 1 H), 7.64 (d, 1 H) 4-532 nPr SOMe Cl 0.99 (t, 3 H), 1.50 (m, 1 H), 1.65 (m, 1 H), 2.97 (m, 1 H), 3.13 (s, 3 H), 3.17 (m, 1 H), 4.11 (s, 3 H), 7.43 (d, 1 H), 7.65 (d, 1 H) 4-533 nPr SO₂Me Cl 0.93 (t, 3 H), 1.68 (m, 2 H), 3.22 (m, 2 H), 3.35 (s, 3 H), 4.12 (s, 3 H), 7.55 (d, 1 H), 7.68 (d, 1 H) 4-534 nPr SMe Br 0.98 (t, 3 H), 1.61 (m, 2 H), 2.42 (s, 3 H), 3.15 (m, 2 H), 4.13 (s, 3 H), 7.52 (d, 1 H), 7.69 (d, 1 H) 4-535 nPr SOMe Br 0.97 (t, 3 H), 1.45 (m, 1 H), 1.60 (m, 1 H), 2.97 (m, 1 H), 3.09 (s, 3 H), 3.12 (m, 1 H), 4.09 (s, 3 H), 7.55 (d, 1 H), 7.63 (d, 1 H) 4-536 nPr SO₂Me Br 0.93 (t, 3 H), 1.65 (m, 2 H), 3.22 (m, 2 H), 3.38 (s, 3 H), 4.12 (s, 3 H), 7.56 (d, 1 H), 7.81 (d, 1 H) 4-537 nPr SMe CF₃ 0.99 (t, 3 H), 1.65 (m, 2 H), 2.34 (s, 3 H), 3.20 (m, 2 H), 4.14 (s, 3 H), 7.74 (s, 2 H), 10.69 (s, 1 H) 4-538 nPr SOMe CF₃ 0.96 (t, 3 H), 1.56 (m, 1 H), 1.70 (m, 1 H), 3.06 (s, 3 H), 3.37 (m, 1 H), 3.57 (m, 1 H), 4.1 (s, 3 H), 7.68 (d, 1 H), 7.79 (d, 1 H) 4-539 nPr SO₂Me CF₃ 0.98 (t, 3S), 1.67 (m, 2 H), 3.25 (m, 2 H), 3.30 (s, 3 H), 4.16 (s, 3 H), 7.91 (s, 2 H), 10.6 (br, s, 1 H) 4-540 nPr SMe SO₂Me 4-541 nPr SOMe SO₂Me 4-542 nPr SO₂Me SO₂Me 4-543 iPr SOMe CF₃ 4-544 iPr SO₂Me CF₃ 1.41 (d, 6 H), 3.32 (s, 3 H), 4.15 (s, 3 H), 4.19 (m, 1 H), 7.78 (d, 1 H), 7.85 (d, 1 H), 10.4 (br, s, 1 H) 4-545 iPr SMe Cl 1.43 (d, 6 H), 2.41 (s, 3 H), 3.89 (br, s, 1 H), 4.12 (s, 3 H), 7.42 (br, m, 2 H), 10.3 (s, 1 H) 4-546 iPr SOMe Cl 1.38 (m, 6 H), 3.09 (s, 3 H), 3.90 (br, s, 1 H), 4.11 (s, 3 H), 7.38 (d, 1 H), 7.51 (d, 1 H) 4-547 iPr SO₂Me Cl 1.21 (d, 6 H), 3.30 (s, 3 H), 3.88 (s, 3 H), 4.27 (m, 1 H), 7.31 (d, 1 H), 7.45 (d, 1 H) 4-548 iPr SMe Br 4-549 iPr SOMe Br 4-550 iPr SO₂Me Br 4-551 iPr SMe SO₂Me 4-552 iPr SOMe SO₂Me 4-553 iPr SO₂Me SO₂Me 4-554 cPr SMe CF₃ 0.72 (m, 1 H), 1.19 (m, 1 H), 2.39 (m, 1 H), 2.48 (s, 3 H), 4.17 (s, 3 H), 7.61 (d, 1 H), 7.71 (d, 1 H), 11.18 (s, 1 H) 4-555 cPr SOMe CF₃ 4-556 cPr SMe Cl 0.63 (m, 1 H), 1.16 (m, 1 H), 2.39 (m, 1 H), 2.51 (s, 3 H), 4.16 (s, 3 H), 7.45 (s, 2 H), 10.59 (s, 1 H) 4-557 cPr SOMe Cl 4-558 cPr SO₂Me Cl 4-559 cPr SMe Br 4-560 cPr SOMe Br 4-561 cPr SO₂Me Br 4-562 cPr SMe SO₂Me 4-563 cPr SOMe SO₂Me 4-564 cPr SO₂Me SO₂Me 0.73 (m, 2 H), 1.05 (m, 2 H), 2.69 (m, 1 H), 3.57 (s, 3 H), 3.67 (s, 3 H), 4.03 (s, 3 H), 8.08 (d, 1 H), 8.24 (d, 1 H), 11.8 (br, s, 1 H) 4-565 CH₂OMe F CF₃ 7.81 (m, 2 H), 4.82 (d, 2 H), 4.10 (s, 3 H), 3.60 (s, 3 H) 4-566 CH₂OMe SMe CF₃ 4-567 CH₂OMe SOMe CF₃ 4-568 CH₂OMe SO₂Me CF₃ 4-569 CH₂OMe SEt CF₃ 4-570 CH₂OMe SOEt CF₃ 4-571 CH₂OMe SO₂Et CF₃ 4-572 CH₂OMe S(CH₂)₂OMe CF₃ 4-573 CH₂OMe SO(CH₂)₂OMe CF₃ 4-574 CH₂OMe SO₂(CH₂)₂OMe CF₃ 4-575 CH₂OMe SMe Cl 4-576 CH₂OMe SOMe Cl 4-577 CH₂OMe SO₂Me Cl 4-578 CH₂OMe SEt Cl 4-579 CH₂OMe SOEt Cl 4-580 CH₂OMe SO₂Et Cl 4-581 CH₂OMe S(CH₂)₂OMe Cl 4-582 CH₂OMe SO(CH₂)₂OMe Cl 4-583 CH₂OMe SO₂(CH₂)₂OMe Cl 4-584 CH₂OMe Cl SO₂Me 8.32 (d, 1 H), 7.88 (d, 1 H), 4.92 (s, 2 H), 4.12 (s, 3 H), 3.61 (s, 3 H), 3.34 (s, 3 H) 4-585 CH₂OMe SMe SO₂Me 4-586 CH₂OMe SOMe SO₂Me 4-587 CH₂OMe SO₂Me SO₂Me 4-588 CH₂OMe SEt SO₂Me 4-589 CH₂OMe SOEt SO₂Me 4-590 CH₂OMe SO₂Et SO₂Me 4-591 CH₂OMe S(CH₂)₂OMe SO₂Me 4-592 CH₂OMe SO(CH₂)₂OMe SO₂Me 4-593 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 4-594 CH₂OMe SMe SO₂Et 4-595 CH₂OMe SOMe SO₂Et 4-596 CH₂OMe SO₂Me SO₂Et 4-597 CH₂OMe SEt SO₂Et 4-598 CH₂OMe SOEt SO₂Et 4-599 CH₂OMe SO₂Et SO₂Et 4-600 CH₂OMe S(CH₂)₂OMe SO₂Et 4-601 CH₂OMe SO(CH₂)₂OMe SO₂Et 4-602 CH₂OMe SO₂(CH₂)₂OMe SO₂Et 4-603 CH₂O(CH₂)₂OEt OEt SO₂Me 8.10 (d, 1 H), 7.75 (d, 1 H), 4.82 (s, 2 H), 4.25 (q, 2 H), 4.08 (s, 3 H), 3.88-3.90 (m, 2 H), 3.59- 3.61 (m, 2 H), 3.36 (q, 2 H), 3.28 (s, 3 H), 1.54 (t, 3 H), 0.91 (t, 3 H) 4-604 CF₃ O(CH₂)₂OEt SO₂Me 8.31 (d, 1 H), 7.87 (d, 1 H), 4.35 (t, 2 H), 3.99 (s, 3 H), 3.80 (t, 2 H), 3.55 (q, 2 H), 3.48 (s, 3 H), 1.16 (t, 3 H) 4-605 CF₃ O(CH₂)₂OEt SO₂Et 12.03 (s, 1 H), 8.30 (d, 1 H), 7.88 (d, 1 H), 4.34 (t, 2 H), 4.00 (s, 3 H), 3.78 (t, 2 H), 3.63 (q, 2 H), 3.54 (q, 2 H), 1.12-1.18 (t, 6 H) 4-606 CF₃ O(CH₂)₂SMe SO₂Me 12.04 (s, 1 H), 8.31 (d, 1 H), 7.88 (d, 1 H), 4.34 (t, 2 H), 4.00 (s, 3 H), 3.48 (s, 3 H), 2.97 (t, 2 H), 2.15 (s, 3 H) 4-607 CF₃ O(CH₂)₂SMe SO₂Et 12.03 (s, 1 H), 8.30 (d, 1 H), 7.89 (d, 1 H), 4.33 (t, 2 H), 4.00 (s, 3 H), 3.60 (q, 2 H), 2.96 (t, 2 H), 2.13 (s, 3 H), 1.13 (t, 3 H) 4-608 CF₃ O(CH₂)₂SEt SO₂Me 12.03 (s, 1 H), 8.31 (d, 1 H), 7.88 (d, 1 H), 4.32 (t, 2 H), 4.00 (s, 3 H), 3.47 (s, 3 H), 3.01 (t, 2 H), 2.60 (q, 2 H), 1.22 (t, 3 H) 4-609 CF₃ O(CH₂)₂SEt SO₂Et 8.30 (d, 1 H), 7.89 (d, 1 H), 4.31 (t, 2 H), 3.97 (s, 3 H), 3.61 (q, 2 H), 2.99 (t, 2 H), 2.60 (q, 2 H), 1.22 (t, 3 H), 1.13 (t, 3 H) 4-610 CF₃ O(CH₂)₃SMe SO₂Me 12.04 (s, 1 H), 8.31 (d, 1 H), 7.87 (d, 1 H), 4.28 (t, 2 H), 4.00 (s, 3 H), 3.44 (s, 3 H), 2.67 (t, 2 H), 2.12 (quin, 2 H), 2.09 (s, 3 H) 4-611 CF₃ O(CH₂)₃SMe SO₂Et 12.05 (s, 1 H), 8.30 (d, 1 H), 7.89 (d, 1 H), 4.27 (t, 2 H), 4.00 (s, 3 H), 3.54 (q, 2 H), 2.65 (t, 2 H), 2.09 (quin, 2 H), 2.08 (s, 3 H), 1.11 (t, 3 H) 4-612 CF₃ oxetan-3-yloxy SO₂Me 12.09 (bs, 1 H), 8.30 (bs, 1 H), 7.89 (bs, 1 H), 5.10-5.15 (m, 1 H), 4.90 (t, 2 H), 4.78 (t, 2 H), 3.99 (s, 3 H), 3.44 (s, 3 H) 4-613 CF₃ oxetan-3-yloxy SO₂Et 12.09 (bs, 1 H), 8.29 (bd, 1 H), 7.90 (bd, 1 H), 5.12-5.15 (m, 1 H), 4.88 (t, 2 H), 4.77 (t, 2 H), 4.00 (s, 3 H), 3.57 (q, 2 H), 1.13 (t, 3 H) 4-614 CF₃ 2-(1H-pyrazol-1- SO₂Et 12.06 (bs, 1 H), 8.28 (d, 1 H), yl)ethoxy 7.90 (d, 1 H), 7.82 (d, 1 H), 4.51 (d, 1 H), 4.29 (t, 1 H), 4.59 (t, 2 H), 4.52 (t, 2 H), 3.99 (s, 3 H), 3.35 (q, 2 H), 1.06 (t, 3 H) 4-615 CF₃ 2-(2-thienyl)ethoxy SO₂Me 12.08 (bs, 1 H), 8.31 (d, 1 H), 7.89 (d, 1 H), 7.41 (d, 1 H), 7.00-7.01 (m, 2 H), 4.41 (t, 2 H), 3.99 (s, 3 H), 3.40 (t, 2 H), 3.32 (s, 3 H) 4-616 CF₃ 2-(2-thienyl)ethoxy SO₂Et 12.03 (bs, 1 H), 8.29 (d, 1 H), 7.89 (d, 1 H), 7.40 (d, 1 H), 7.00-7.02 (m, 2 H), 4.40 (t, 2 H), 4.00 (s, 3 H), 3.37-3.42 (m, 4 H), 1.08 (t, 3 H) 4-617 CF₃ 1,3-dioxolan-4- SO₂Me 12.11 (bs, 1 H), 8.35 (d, 1 H), ylmethoxy 7.86 (bs, 1 H), 4.85 (d, 1 H), 4.75 (d, 1 H), 4.51-4.53 (m, 1 H), 4.10-4.13 (m, 2 H), 3.99 (s, 3 H), 3.97-4.00 (m, 2 H), 3.48 (s, 3 H) 4-618 CF₃ 1,3-dioxolan-4- SO₂Et 12.09 (bs, 1 H), 8.34 (d, 1 H), ylmethoxy 7.89 (d, 1 H), 4.85 (d, 1 H), 4.75 (d, 1 H), 4.51-4.54 (m, 1 H), 4.10-4.12 (m, 2 H), 4.00 (s, 3 H), 3.96-4.01 (m, 2 H), 3.57-3.63 (m, 2 H), 1.11 (t, 3 H) 4-619 CF₃ tetrahydrofuran-3- SO₂Me 12.09 (bs, 1 H), 8.32 (bd, 1 H), ylmethoxy 7.89 (bs, 1 H), 4.12-4.18 (m, 2 H), 4.00 (s, 3 H), 3.81-3.84 (m, 1 H), 3.77-3.80 (m, 1 H), 3.62- 3.69 (m, 2 H), 3.42 (s, 3 H), 2.78-2.82 (m, 1 H), 2.03-2.09 (m, 1 H), 1.68-1.72 (m, 1 H) 4-620 CF₃ tetrahydro-2H-pyran- SO₂Me 12.07 (bs, 1 H), 8.31 (bd, 1 H), 2-ylmethoxy 7.87 (bs, 1 H), 4.26 (dd, 1 H), 4.08 (dd, 1 H), 3.99 (s, 3 H), 3.93-3.95 (m, 1 H), 3.75-3.78 (m, 1 H), 3.49 (s, 3 H), 3.42-3.46 (m, 1 H), 1.80-1.85 (m, 1 H), 1.60-1.64 (m, 1 H), 1.49-1.55 (m, 3 H), 1.29-1.35 (m, 1 H) 4-621 CF₃ tetrahydro-2H-pyran- SO₂Et 12.06 (bs, 1 H), 8.30 (bs, 1 H), 2-ylmethoxy 7.89 (bs, 1 H), 4.24 (dd, 1 H), 4.06 (dd, 1 H), 4.00 (s, 3 H), 3.91-3.95 (m, 1 H), 3.72-3.77 (m, 1 H), 3.59-3.65 (m, 2 H), 3.40-3.45 (m, 1 H), 1.80-1.84 (m, 1 H), 1.60-1.63 (m, 1 H), 1.48-1.55 (m, 3 H), 1.25-1.33 (m, 1 H), 1.11 (t, 3 H) 4-622 CF₃ SOMe SO₂Me 12.02 (bs, 1 H), 8.49 (d, 1 H), 8.15 (d, 1 H), 4.01 (s, 3 H), 3.62 (s, 3 H), 3.31 (s, 3 H) 4-623 F SO₂Me CF₃ 12.05 (brs, 1 H), 8.32 (t, 1 H), 8.07 (d, 1 H), 4.00 (s, 3 H), 3.52 (d, 3 H) 4-624 F SCH₂Ph CF₃ 8.12 (t, 1 H), 7.69 (d, 1 H), 7.30- 7.23 (m, 3 H), 7.23-7.21 (m, 2 H), 4.13 (s, 2 H), 4.08 (s, 3 H) 4-625 F SMe F 8.11 (m, 1 H), 7.14 (t, 1 H), 4.07 (s, 3 H), 2.53 (s, 3 H) 4-626 F SOMe F 8.24 (m, 1 H), 7.27-7.12 (m, 1 H), 4.07 (s, 3 H), 3.23 (s, 3 H) 4-627 F SO₂Me F 8.38 (m, 1 H), 7.32-7.20 (m, 1 H), 4.07 (s, 3 H), 3.42 (s, 3 H) 4-628 Cl SO₂Me H 8.41 (d, 1 H), 7.96 (d, 1 H), 7.68 (t, 1 H), 4.14 (s, 3 H), 3.34 (s, 3 H) 4-629 Cl SCF₂CF₂H H 7.98 (d, 1 H), 7.84 (d, 1 H), 7.48 (t, 1 H), 5.91 (tt, 1 H), 4.13 (s, 3 H) 4-630 Cl SOCF₂CF₂H H 8.20 (d, 1 H), 8.06 (dd, 1 H), 7.79 (t, 1 H), 6.27 (ddt, 1 H), 4.14 (s, 3 H) 4-631 Cl SO₂CF₂CF₂H H 8.37 (d, 1 H), 8.07 (dd, 1 H), 7.75 (t, 1 H), 6.33 (tt, 1 H), 4.15 (s, 3 H) 4-632 Cl SMe Me 9.89 (bs, 1 H), 7.59 (d, 1 H), 7.32 (d, 1 H), 4.12 (s, 3 H), 2.66 (s, 3 H), 2.38 (s, 3 H) 4-633 Cl SOMe Me 11.84 (bs, 1 H), 7.76 (d, 1 H), 7.46 (d, 1 H), 3.99 (s, 3 H), 3.02 (s, 3 H), 2.72 (s, 3 H) 4-634 Cl SO₂Me Me 11.87 (bs, 1 H), 7.88 (d, 1 H), 7.57 (d, 1 H), 4.01 (s, 3 H), 3.42 (s, 3 H), 2.75 (s, 3 H) 4-635 Cl SEt Me 9.68 (bs, 1 H), 7.59 (d, 1 H), 7.33 (d, 1 H), 4.12 (s, 3 H), 4.88 (q, 2 H), 2.65 (s, 3 H), 1.22 (t, 3 H) 4-636 Cl SOEt Me 7.65 (d, 1 H), 7.28 (d, 1 H), 4.11 (s, 3 H), 3.25-3.30 (m, 1 H), 3.10-3.15 (m, 1 H), 2.70 (s, 3 H), 1.40 (t, 3 H) 4-637 Cl SO₂Et Me 7.70 (d, 1 H), 7.41 (d, 1 H), 4.13 (s, 3 H), 3.49 (q, 2 H), 2.84 (s, 3 H), 1.36 (t, 3 H) 4-638 Cl SMe CF₃ 7.78 (d, 1 H), 7.69 (d, 1 H), 3.78 (s, 3 H), 2.40 (s, 3 H) 4-639 Cl SOMe CF₃ 4-640 Cl SO₂Me CF₃ 12.03 (s, 1 H), 8.11 (d, 1 H), 8.08 (d, 1 H), 4.03 (s, 3 H), 3.16 (s, 3 H) 4-641 Cl CF₃ Cl 12.24 (s, 1 H), 8.06 (d, 1 H), 7.90 (d, 1 H), 4.03 (s, 3 H) 4-642 Cl CH₂(4-methoxy-3- Cl 11.87 (brs, 1 H), 7.75 (d, 1 H), isopropoxy-1,2,4- 7.68 (d, 1 H), 5.09 (s, 2 H), 4.72 triazolin-5-on-1-yl) (m, 1 H), 4.00 (s, 3 H), 2.99 (s, 3 H), 1.27 (d, 6 H) 4-643 Cl CH₂(4-methyl-3- Cl 11.88 (brs, 1 H), 7.76 (d, 1 H), trifluoroethoxy-1,2,4- 7.68 (d, 1 H), 5.12 (s, 2 H), 4.83 triazolin-5-on-1-yl) (q, 2 H), 4.00 (s, 3 H), 3.07 (s, 3 H) 4-644 Cl CH₂(4-methyl-3- Cl 2.41 (s, 3 H), 3.13 (s, 3 H), 3.99 (methylsulfanyl)-5- (s, 3 H), 5.16 (s, 2 H), 7.69 oxo-4,5-dihydro-1H- (d, 1 H), 7.77 (d, 1 H) 1,2,4-triazol-1-yl) 4-645 Cl CH₂(4-isopropylyl-3- Cl 1.31 (d, 6 H), 3.06 (s, 3 H), 4.10 (methylsulfanyl)-5- (s, 3 H), 4.85 (m, 1 H), 5.14 oxo-4,5-dihydro-1H- (s, 2 H), 7.48 (d, 1 H), 7.61 1,2,4-triazol-1-yl) (d, 1 H), 10.70 (br, s, 1 H) 6-646 Cl CH₂(3- Cl 2.73 (s, 6 H), 3.24 (s, 3 H), 4.08 (dimethoxyamino)-4- (s, 3 H), 5.25 (s, 2 H), 7.61 methyl-5-oxo-4,5- (d, 1 H), 7.66 (d, 1 H) dihydro-1H-1,2,4- triazol-1-yl) 4-647 Cl CH₂(3-oxo-5,6,7,8- Cl 1.85 (m, 2 H), 1.96 (m, 2 H), 2.61 tetrahydro[1,2,4]triazolo (t, 2 H), 3.62 (t, 2 H), 4.08 (s, 3 H), [4,3-a]pyridin- 5.29 (s, 2 H), 7.62 (d, 1 H), 7.67 2(3H)-yl) (d, 1 H) 4-648 Cl CH₂(4-cyclopropyl-3- Cl 0.86 (m, 4 H), 1.85 (m, 2 H), 2.70 methoxy-5-oxo-4,5- (m, 1 H), 3.78 (s, 3 H), 3.99 dihydro-1H-1,2,4- (s, 3 H), 5.05 (s, 2 H), 7.68 triazol-1-yl) (d, 1 H), 7.76 (d, 1 H), 11.90 (s, 1 H) 4-649 Cl CH₃(3-methyl-6- Cl 3.43 (s, 3 H), 3.99 (s, 3 H), 5.80 oxopyridazin-1(6H)- (s, 2 H), 6.94 (d, 1 H), 7.32 yl) (d, 1 H), 8.02 (d, 1 H), 8.19 (d, 1 H), 12.04 (s, 1 H) 4-650 Cl CH₂(6-oxopyridazin- Cl 4.11 (s, 3 H), 5.58 (s, 2 H), 6.95 1(6H)-yl) (dd, 1 H), 7.19 (dd, 1 H), 7.49 (d, 1 H), 7.65 (d, 1 H), 7.67 (dd, 1 H), 11.1 (s, 1 H) 4-651 Cl CH₂(4-cyclopropyl-5- Cl 0.85 (m, 2 H), 0.91 (m, 2 H), 2.78 oxo-3-(2,2,2- (m, 1 H), 3.98 (s, 3 H), 4.82 trifluoroethoxy)-4,5- (q, 2 H), 5.07 (s, 2 H), 7.66 dihydro-1H-1,2,4- (d, 1 H), 7.73 (d, 1 H), 11.85 triazol-1-yl) (s, 1 H) 4-652 Cl CH₂(3-methoxy-4- Cl 3.02 (s, 3 H), 3.80 (s, 3 H), 3.98 methyl-5-oxo-4,5- (s, 3 H), 5.09 (s, 2 H), 7.67 dihydro-1H-1,2,4- (d, 1 H), 7.73 (d, 1 H), 11.9 (s, 1 H) triazol-1-yl) 4-653 Cl CH₂(3,4- Cl 0.78 (m, 2 H), 0.92 (m, 2 H), 1.02 dicyclopropyl-5-oxo- (m, 2 H), 1.08 (m, 2 H), 1.96 4,5-dihydro-1H-1,2,4- (m, 1 H), 2.89 (m, 1 H), 3.95 triazol-1-yl) (s, 3 H), 5.18 (s, 2 H), 7.46 (d, 1 H), 7.65 (d, 1 H) 4-654 Cl CH₂(3-ethoxy-4- Cl 1.27 (t, 3 H), 3.01 (s, 3 H), 3.99 methyl-5-oxo-4,5- (s, 3 H), 5.08 (s, 2 H), 7.67 dihydro-1H-1,2,4- (d, 1 H), 7.74 (d, 1 H), 11.89 triazol-1-yl) (s, 1 H) 4-655 Cl NHCH₂CONHEt Cl 11.74 (brs, 1 H), 8.10 (t, 1 H), 7.39 (d, 1 H), 7.14 (d, 1 H), 5.7 (brs, 1 H), 3.98 (d, 2 H), 3.94 (s, 3 H), 3.14 (m, 2 H), 1.03 (t, 3 H) 4-656 Cl NHCH(CH₃)CONHEt Cl 1.15 (t, 3 H), 1.44 (d, 3 H), 3.33 (m, 2 H), 4.10 (s, 3 H), 4.10 (m, 1 H), 4.51 (d, br, 1 H), 6.84 (t, 1 H), 7.24 (d, 1 H), 7.40 (d, 1 H), 11.20 (s, 1 H) 4-657 Cl NHCH₂CONHiPr Cl 1.19 (d, 6 H), 3.84 (d, 2 H), 4.11 (s, 3 H), 4.12 (m, 1 H), 4.90 (t, 1 H), 6.50 (d, 1 H), 7.23 (d, 1 H), 7.39 (d, 1 H), 10.91 (s, 1 H) 4-658 Cl NHCH(Me)CONH₂ Cl 1.74 (d, 3 H), 4.11 (s, 3 H), 4.30 (d, 1 H), 4.73 (m, 1 H), 7.41 (d, 1 H), 7.49 (d, 1 H), 10.7 (s, 1 H) 4-659 Cl NHAc Cl 7.70 (s, 1 H), 7.68 (d, 1 H), 7.61 (d, 1 H), 4.00 (s, 3 H), 2.10 (s, 3 H) 4-660 Cl NHCONMe₂ Cl 4-661 Cl OMe Cl 11.85 (bs, 1 H), 7.69 (d, 1 H), 7.56 (d, 1 H), 4.00 (s, 3 H), 3.88 (s, 3 H) 4-662 Cl OEt Cl 11.85 (bs, 1 H), 7.68 (d, 1 H), 7.54 (d, 1 H), 4.10 (q, 2 H), 3.99 (s, 3 H), 1.41 (t, 3 H) 4-663 Cl O(CH₂)₃SMe Cl 11.00 (bs, 1 H), 7.45 (d, 1 H), 7.44 (d, 1 H), 4.17 (t, 2 H), 4.08 (s, 3 H), 2.80 (t, 2 H), 2.16 (quin, 2 H), 2.16 (s, 3 H) 4-664 Cl O(CH₂)₂SEt Cl 7.41 (bs, 2 H), 4.21 (t, 2 H), 4.06 (s, 3 H), 3.01 (t, 2 H), 2.65 (q, 2 H), 1.30 (t, 3 H) 4-665 Cl O(CH₂)₂SMe Cl 11.18 (bs, 1 H), 7.47 (d, 1 H), 7.46 (d, 1 H), 4.26 (t, 2 H), 4.10 (s, 3 H), 2.99 (t, 2 H), 2.22 (s, 3 H) 4-666 Cl O(CH₂)₃OMe Cl 11.85 (bs, 1 H), 7.68 (d, 1 H), 7.54 (d, 1 H), 4.08 (t, 2 H), 3.99 (s, 3 H), 3.56 (t, 2 H), 3.27 (s, 3 H), 2.03 (quin, 2 H) 4-667 Cl cyclopropylmethoxy Cl 11.85 (bs, 1 H), 7.67 (d, 1 H), 7.53 (d, 1 H), 3.99 (s, 3 H), 3.90 (d, 2 H), 1.25-1.33 (m, 1 H), 0.58-0.60 (m, 2 H), 0.33-0.36 (m, 2 H) 4-668 Cl 1,4-dioxan-2- Cl 10.98 (bs, 1 H), 7.45-7.51 (m, ylmethoxy 2 H), 3.99-4.18 (m, 7 H), 3.60- 3.90 (m, 5 H) 4-669 Cl tetrahydrofuran-1- Cl 11.85 (bs, 1 H), 7.68 (d, 1 H), ylmethoxy 7.52 (d, 1 H), 4.20-4.26 (m, 1 H), 4.04 (dd, 1 H), 3.99 (s, 3 H), 3.97 (dd, 1 H), 3.80 (dd, 1 H), 3.70 (dd, 1 H), 2.00-2.05 (m, 1 H), 1.77-1.90 (m, 3 H) 4-670 Cl Br Cl 11.90 (s, 1 H), 7.80 (d, 1 H), 7.77 (d, 1 H), 3.98 (s, 3 H) 4-671 Cl SO₂Me Cl 7.71 (d, 1 H), 7.63 (d, 1 H), 4.11 (s, 3 H), 3.40 (s, 3 H) 4-672 Cl SOMe Cl 7.71 (d, 1 H), 7.51 (d, 1 H), 4.11 (s, 3 H), 3.11 (s, 3 H) 4-673 Cl SMe Cl 7.61 (d, 1 H), 7.55 (d, 1 H), 4.13 (s, 3 H), 2.48 (s, 3 H) 4-674 Cl SEt Cl 7.60 (d, 1 H), 7.55 (d, 1 H), 4.12 (s, 3 H), 2.98 (q, 2 H), 1.25 (t, 3 H) 4-675 Cl SOEt Cl 7.70 (d, 1 H), 7.51 (d, 1 H), 4.11 (s, 3 H), 3.49 (m, 1 H), 3.28 (m, 1 H), 1.39 (t, 3 H) 4-676 Cl SO₂Et Cl 8.02 (d, 1 H), 7.89 (d, 1 H), 4.01 (s, 3 H), 3.62 (q, 2 H), 1.25 (t, 3 H) 4-677 Cl S(CH₂)₂OMe Cl 7.60 (d, 1 H), 7.55 (d, 1 H), 4.12 (s, 3 H), 3.56 (t, 2 H), 3.32 (s, 3 H), 3.13 (t, 2 H) 4-678 Cl SO(CH₂)₂OMe Cl 7.68 (d, 1 H), 7.49 (d, 1 H), 4.10 (s, 3 H), 3.89 (m, 1 H), 3.73 (m, 1 H), 3.66 (m, 1 H), 3.36 (m, 1 H), 3.36 (s, 3 H) 4-679 Cl SO₂(CH₂)₂OMe Cl 7.69 (d, 1 H), 7.62 (d, 1 H), 4.13 (s, 3 H), 3.88 (t, 2 H), 3.73 (t, 2 H), 3.22 (s, 3 H) 4-680 Cl OMe Br 11.85 (bs, 1 H), 7.81 (d, 1 H), 7.47 (d, 1 H), 3.99 (s, 3 H), 3.86 (s, 3 H), 4-681 Cl OEt Br 11.85 (bs, 1 H), 7.82 (d, 1 H), 7.47 (d, 1 H), 4.09 (q, 2 H), 3.99 (s, 3 H), 1.42 (t, 3 H) 4-682 Cl O(CH₂)₂OMe Br 11.00 (bs, 1 H), 7.63 (d, 1 H), 7.41 (d, 1 H), 4.26 (t, 2 H), 4.10 (s, 3 H), 3.84 (t, 2 H), 3.27 (s, 3 H) 4-683 Cl O(CH₂)₃OMe Br 11.85 (bs, 1 H), 7.81 (d, 1 H), 7.45 (d, 1 H), 4.07 (t, 2 H), 3.99 (s, 3 H), 3.56 (t, 2 H), 3.27 (s, 3 H), 2.04 (quin, 2 H) 4-684 Cl OCH₂(CO)NMe₂ Br 11.90 (bs, 1 H), 7.82 (d, 1 H), 7.50 (d, 1 H), 4.71 (s, 2 H), 3.99 (s, 3 H), 3.01 (s, 3 H), 2.88 (s, 3 H) 4-685 Cl tetrahydrofuran-2- Br 11.85 (br, 1 H), 7.81 (d, 1 H), ylmethoxy 7.46 (d, 1 H), 4.22-4.28 (m, 1 H), 4.00-4.03 (m, 1 H), 3.99 (s, 3 H), 3.92 (dd, 1 H), 3.79-3.82 (m, 1 H), 3.68-3.72 (m, 1 H), 2.00-2.05 (m, 1 H), 1.80-1.92 (m, 3 H) 4-686 Cl 1,4-dioxan-2- Br 10.80 (bs, 1 H), 7.64 (d, 1 H), ylmethoxy 7.43 (d, 1 H), 4.00-4.18 (m, 7 H), 3.60-3.90 (m, 5 H) 4-687 Cl Me SMe 11.66 (brs, 1 H), 7.56 (d, 1 H), 7.31 (d, 1 H), 3.99 (s, 3 H), 2.56 (s, 3 H), 2.39 (s, 3 H) 4-688 Cl Me SO₂Et 8.10 (d, 1 H), 7.64 (d, 1 H), 4.19 (s, 3 H), 3.23 (q, 2 H), 2.81 (s, 3 H), 1.31 (t, 3 H) 4-689 Cl CH₂N(Me)COEt SO₂Me 4-690 Cl CH₂OC₂H₄OMe SO₂Me 3.31 (s, 3 H), 3.34 (s, 3 H), 3.58 (m, 2 H), 3.79 (m, 2 H), 4.13 (s, 3 H), 5.19 (s, 2 H), 7.78 (d, 1H), 8.14 (d, 1 H), 10.65 (s, 1 H) 4-691 Cl CH₂OC₂H₄OEt SO₂Me 1.16 (t, 3 H), 3.32 (s, 3 H), 3.50 (q, 2 H), 3.62 (m, 2 H), 3.80 (m, 2 H), 4.11 (s, 3 H), 5.19 (s, 2 H), 7.77 (d, 1 H), 8.12 (d, 1 H), 10.5 (s, 1 H) 4-692 Cl CH₂OCH₂iPr SO₂Me 0.92 (d, 6 H), 1.90 (m, 1 H), 3.29 (s, 3 H), 3.43 (d, 2 H), 4.15 (s, 3 H), 5.12 (s, 2 H), 7.80 (d, 1 H), 8.18 (d, 1 H), 10.42 (s, 1 H) 4-693 Cl CH₂OCH₂CF₃ SMe 11.74 (brs, 1 H), 7.71 (d, 1 H), 7.45 (d, 1 H), 4.92 (s, 2 H), 4.18 (q, 2 H), 3.99 (s, 3 H), 2.57 (s, 3 H) 4-694 Cl CH2OCH₂cPr SO₂Me 0.25 (m, 2 H), 0.58 (m, 2 H), 3.33 (s, 3 H), 3.48 (d, 2 H), 4.14 (s, 3 H), 5.15 (s, 2 H), 7.80 (d, 1 H), 8.15 (d, 1 H), 10.83 (s, 1 H) 4-695 Cl CO₂H SO₂Me 12.04 (brs, 1 H), 8.01 (d, 1 H), 8.07 (d, 1 H), 4.02 (s, 3 H), 3.35 (s, 3 H) 4-696 Cl NHnPr SO₂Me 1.02 (t, 3 H), 1.70 (m, 2 H), 3.15 (s, 3 H), 3.50 (t, br, 2 H), 4.14 (s, 3 H), 5.87 (s, br, 1 H), 7.11 (d, 1 H), 7.87 (d, 1 H), 11.11 (s, 1 H) 4-697 Cl NHCH₂cPr SO₂Me 0.30 (m, 2 H), 0.61 (m, 2 H), 1.13 (m, 1 H), 3.16 (s, 3 H), 3.39 (d, 2 H), 4.14 (s, 3 H), 5.99 (s, br, 1 H), 7.12 (d, 1 H), 7.88 (d, 1 H), 11.0 (s, br, 1 H) 4-698 Cl NHCH₂CH₂OMe SO₂Me 3.23 (s, 3 H), 3.39 (s, 3 H), 3.6 (m, 2 H), 3.71 (m, 2 H), 4.13 (s, 3 H), 6.04 (t, br, 1 H), 7.15 (d, 1 H), 7.88 (d, 1 H), 10.89 (s, br, 1 H) 4-699 Cl NHCH₂CH₂OEt SO₂Me 1.22 (t, 3 H), 3.23 (s, 3 H), 3.55 (q, 2 H), 3.65 (m, 2 H), 3.72 (m, 2 H), 4.13 (s, 3 H), 6.09 (t, 1 H), 7.15 (d, 1 H), 7.88 (d, 1 H), 10.79 (s, 1 H) 4-700 Cl NHCH₂CH₂CH₂OMe SO₂Me 1.94 (m, 2 H), 3.17 (s, 3 H), 3.38 (s, 3 H), 3.54 (m, 2 H), 3.64 (m, 2 H), 4.14 (s, 3 H), 5.95 (t, br, 1 H), 7.15 (d, 1 H), 7.90 (d, 1 H), 10.3 (s, br, 1 H) 4-701 Cl NHCH₂CH₂OCOiPr SO₂Me 1.20 (d, 6 H), 2.49 (s, 3 H), 2.62 (m, 1 H), 3.13 (s, 3 H), 3.52 (m, 2 H), 4.11 (s, 3 H), 4.31 (m, 2 H), 5.82 (t, br, 1 H), 7.34 (d, 1 H), 7.84 (d, 1 H), 11.01 (s, 1 H) 4-702 Cl NHCH₂CH₂OCOcPr SO₂Me 0.9 (m, 2 H), 1.04 (m, 2 H), 1.66 (m, 1 H), 2.49 (s, 3 H), 3.15 (s, 3 H), 3.51 (s, br, 2 H), 4.12 (s, 3 H), 4.31 (t, 2 H), 5.83 (t, br, 1 H), 7.33 (d, 1 H), 7.84 (d, 1 H), 10.82 (s, 1 H) 4-703 Cl pyrazol-1-yl SO₂Me 4-704 Cl 4-Me-pyrazol-1-yl SO₂Me 8.15 (s, 1 H), 8.15 (d, 1 H), 8.07 (d, 1 H), 3.91 (s, 3 H), 3.16 (s, 3 H), 2.12 (s, 3 H) 4-705 Cl 4-MeO-pyrazol-1-yl SO₂Me 4-706 Cl 4-CN-pyrazol-1-yl SO₂Me 4-707 Cl 4-Cl-pyrazol-1-yl SO₂Me 4-708 Cl 3,5-Me₂-pyrazol-1-yl SO₂Me 8.12 (b, 1 H), 8.05 (b, 1 H), 6.59 (s, 1 H), 3.68 (s, 3 H), 3.21 (s, 3 H), 2.18 (s, 6 H) 4-709 Cl 1,2,4-triazol-1-yl SO₂Me 4-710 Cl 5-iPR-1,2,4-triazol-1-yl SO₂Me 12.14 (s, 1 H), 8.76 (s, 1 H), 8.18 (d, 1 H), 8.12 (d, 1 H), 3.89 (s, 3 H), 3.25 (s, 3 H), 3.07 (m, 1 H), 1.29 (d, 6 H) 4-711 Cl 5-EtS-1,2,4-triazol- SO₂Me 12.21 (s, 1 H), 8.93 (s, 1 H), 1-yl 8.22 (bs, 2 H), 3.97 (s, 1 H), 3.27 (s, 3 H), 3.11 (q, 2 H), 1.33 (t, 3 H) 4-712 Cl OPr SO₂Me 11.97 (s, 1 H), 7.94 (d, 1 H), 7.75 (d, 1 H), 4.16 (t, 2 H), 4.01 (s, 3 H), 3.39 (s, 3 H), 1.89 (sex, 2 H), 1.05 (t, 3 H) 4-713 Cl OPr SO₂Et 11.00 (bs, 1 H), 8.00 (d, 1 H), 7.59 (d, 1 H), 4.24 (t, 2 H), 4.14 (s, 3 H), 3.47 (q, 2 H), 1.95 (quin, 2 H), 1.28 (t, 3 H), 1.09 (t, 3 H) 4-714 Cl isobutoxy SO₂Me 10.40 (bs, 1 H), 8.04 (d, 1 H), 7.61 (d, 1 H), 4.28 (d, 2 H), 4.14 (s, 3 H), 3.30 (s, 3 H), 2.28 (sep, 1 H), 1.11 (s, 3 H), 1.09 (s, 3 H) 4-715 Cl butoxy SO₂Me 10.22 (bs, 1 H), 8.04 (d, 1 H), 7.61 (d, 1 H), 4.30 (t, 2 H), 4.14 (s, 3 H), 3.29 (s, 3 H), 1.89-1.96 (m, 2 H), 1.51-1.60 (m, 2 H), 0.88 (t, 3 H) 4-716 Cl isohexyloxy SO₂Me 10.09 (bs, 1 H), 8.04 (d, 1 H), 7.61 (d, 1 H), 4.32 (t, 2 H), 4.14 (s, 3 H), 3.29 (s, 3 H), 1.82-1.86 (m, 3 H), 1.50-1.60 (m, 2 H), 1.02 (s, 3 H), 1.00 (s, 3 H) 4-717 Cl allyloxy SO₂Me 12.01 (bs, 1 H), 7.96 (d, 1 H), 7.79 (d, 1 H), 6.20 (m, 1 H), 5.51 (d, 1 H), 5.37 (d, 1 H), 4.70-4.72 (m, 2 H), 4.02 (s, 3 H), 3.39 (s, 3 H) 4-718 Cl allyloxy SO₂Et 12.01 (bs, 1 H), 7.93 (d, 1 H), 7.80 (d, 1 H), 6.12-6.22 (m, 1 H), 5.51 (d, 1 H), 5.35 (d, 1 H), 4.69-4.72 (m, 2 H), 4.02 (s, 3 H), 3.50 (q, 2 H), 1.12 (t, 3 H) 4-719 Cl propargyloxy SO₂Et 10.65 (bs, 1 H), 8.03 (d, 1 H), 7.66 (d, 1 H), 4.97 (d, 2 H), 4.14 (s, 3 H), 3.51 (q, 2 H), 2.67 (t, 1 H), 1.29 (t, 3 H) 4-720 Cl propargyloxy SO₂Me 10.35 (bs, 1 H), 8.05 (d, 1 H), 7.67 (d, 1 H), 4.98 (d, 2 H), 4.14 (s, 3 H), 3.34 (s, 3 H), 2.68 (t, 1 H) 4-721 Cl OCH₂CH₂F SO₂Me 9.80 (bs, 1 H), 8.05 (d, 1 H), 7.67 (d, 1 H), 4.93 (dd, 1 H), 4.81 (dd, 1 H), 4.62 (dd, 1 H), 4.55 (dd, 1 H), 4.14 (s, 3 H), 3.33 (s, 3 H) 4-722 Cl OCH₂CH₂F SO₂Et 10.70 (bs, 1 H), 8.05 (d, 1 H), 7.66 (d, 1 H), 4.90 (bs, 1 H), 4.82 (bs, 1H), 4.59 (bs, 1 H), 4.54 (bs, 1 H), 4.15 (s, 3 H), 3.51 (q, 2 H), 1.29 (t, 3 H) 4-723 Cl OCH₂CF₃ SO₂Me 4-724 Cl OCH₂CF₃ SO₂Et 10.90 (bs, 1 H), 8.06 (d, 1 H), 7.71 (d, 1 H), 4.72 (q, 2 H), 4.15 (s, 3 H), 3.47 (q, 2 H), 1.30 (t, 3 H) 4-725 Cl OCH₂CN SO₂Me 11.00 (bs, 1 H), 8.06 (d, 1 H), 7.73 (d, 1 H), 5.08 (s, 2 H), 5.15 (s, 3 H), 3.32 (s, 3 H) 4-726 Cl OCH₂CN SO₂Et 11.60 (bs, 1 H), 8.03 (d, 1 H), 7.71 (d, 1 H), 5.08 (s, 2 H), 4.16 (s, 3 H), 3.46 (q, 2 H), 1.33 (t, 3 H) 4-727 Cl O(CH₂)₂OEt SO₂Me 10.33 (bs, 1 H), 8.05 (d, 1 H), 7.64 (d, 1 H), 4.48 (t, 2 H), 4.14 (s, 3 H), 3.91 (t, 2 H), 3.64 (q, 2 H), 3.36 (s, 3 H), 1.27 (t, 3 H) 4-728 Cl O(CH₂)₂OEt SO₂Et 10.36 (bs, 1 H), 8.04 (d, 1 H), 7.63 (d, 1 H), 4.46 (t, 2 H), 4.14 (s, 3 H), 3.90 (t, 2 H), 3.64 (q, 2 H), 3.55 (q, 2 H), 1.27 (t, 3 H), 1.27 (t, 3 H) 4-729 Cl O(CH₂)₂OCF₃ SO₂Me 10.81 (bs, 1 H), 8.07 (d, 1 H), 7.67 (d, 1 H), 4.56-4.58 (m, 2 H), 4.43-4.45 (m, 2 H), 4.15 (s, 3 H), 3.32 (s, 3 H) 4-730 Cl O(CH₂)₂OCF₃ SO₂Et 10.80 (bs, 1 H), 8.05 (d, 1 H), 7.66 (d, 1 H), 4.54-4.57 (m, 2 H), 4.41-4.44 (m, 2 H), 4.15 (s, 3 H), 3.48 (q, 2 H), 1.30 (t, 3 H) 4-731 Cl O(CH₂)₃OCF₃ SO₂Me 10.64 (bs, 1 H), 8.06 (d, 1 H), 7.65 (d, 1 H), 4.42 (t, 2 H), 4.27 (t, 2 H), 4.14 (s, 3 H), 3.27 (s, 3 H), 2.33 (quin, 2 H) 4-732 Cl O(CH₂)₃OCF₃ SO₂Et 10.88 (bs, 1 H), 8.03 (d, 1 H), 7.63 (d, 1 H), 4.41 (t, 2 H), 4.26 (t, 2 H), 4.14 (s, 3 H), 3.42 (q, 2 H), 2.31 (quin, 2 H), 1.29 (t, 3 H) 4-733 Cl O(CH₂)₂SMe SO₂Me 12.00 (bs, 1 H), 7.96 (d, 1 H), 7.78 (d, 1 H), 4.32 (t, 2 H), 4.02 (s, 3 H), 3.45 (s, 3 H), 3.01 (t, 2 H), 2.16 (s, 3 H) 4-734 Cl O(CH₂)₂SMe SO₂Et 12.00 (bs, 1 H), 7.94 (d, 1 H), 7.79 (d, 1 H), 4.31 (t, 2 H), 4.02 (s, 3 H), 3.59 (q, 2 H), 3.48 (q, 2 H), 3.00 (t, 2 H), 2.16 (s, 3 H), 1.13 (t, 3 H), 1.12 (t, 3 H) 4-735 Cl O(CH₂)₂SEt SO₂Me 12.00 (bs, 1 H), 7.95 (d, 1 H), 7.78 (d, 1 H), 4.30 (t, 2 H), 4.02 (s, 3 H), 3.44 (s, 3 H), 3.04 (t, 2 H), 2.63 (q, 2 H), 1.23 (t, 3 H) 4-736 Cl O(CH₂)₂SEt SO₂Et 12.00 (bs, 1 H), 7.93 (d, 1 H), 7.79 (d, 1 H), 4.29 (t, 2 H), 4.02 (s, 3 H), 3.58 (q, 2 H), 3.03 (t, 2 H), 2.62 (q, 2 H), 1.22 (t, 3 H), 1.13 (t, 3 H) 4-737 Cl O(CH₂)₃SMe SO₂Me 12.01 (bs, 1 H), 7.95 (d, 1 H), 7.75 (d, 1 H), 4.27 (t, 2 H), 4.01 (s, 3 H), 3.39 (s, 3 H), 2.70 (t, 2 H), 2.15 (quin, 2 H), 2.10 (s, 3 H) 4-738 Cl O(CH₂)₃SMe SO₂Et 10.90 (bs, 1 H), 7.93 (d, 1 H), 7.76 (d, 1 H), 4.26 (t, 2 H), 4.01 (s, 3 H), 3.51 (q, 2 H), 2.69 (t, 2 H), 2.13 (quin, 2 H), 2.09 (s, 3 H), 1.13 (t, 3 H) 4-739 Cl O(CH₂)₃SEt SO₂Me 12.00 (bs, 1 H), 7.95 (d, 1 H), 7.75 (d, 1 H), 4.27 (t, 2 H), 4.00 (s, 3 H), 3.40 (s, 3 H), 2.73 (t, 2 H), 2.57 (q, 2 H), 2.13 (quin, 2 H), 1.20 (t, 3 H) 4-740 Cl OCH₂(CO)OEt SO₂Me 12.02 (bs, 1 H), 7.96 (d, 1 H), 7.82 (d, 1 H), 4.80 (s, 2 H), 4.25 (q, 2 H), 4.01 (s, 3 H), 3.48 (s, 3 H), 1.26 (t, 3 H) 4-741 Cl OCH₂(CO)OEt SO₂Et 12.01 (bs, 1 H), 7.94 (d, 1 H), 7.83 (d, 1 H), 4.78 (s, 2 H), 4.23 (q, 2 H), 4.01 (s, 3 H), 3.62 (q, 2 H), 1.25 (t, 3 H), 1.13 (t, 3 H) 4-742 Cl Cyclopropylmethoxy SO₂Me 8.04 (d, 1 H), 7.61 (d, 1 H), 4.14 (s, 3 H), 4.03-4.16 (m, 2 H), 3.35 (s, 3 H), 1.45-1.51 (m, 1 H), 0.64-0.72 (m, 2 H), 0.42-0.50 (m, 2 H) 4-743 Cl Cyclopropylmethoxy SO₂Et 10.20 (bs, 1 H), 8.02 (d, 1 H), 7.62 (d, 1 H), 4.14 (s, 3 H), 4.12 (d, 2 H), 3.54 (q, 2 H), 1.40-1.50 (m, 1 H), 1.28 (t, 3 H), 0.68-0.70 (m, 2 H), 0.48-0.50 (m, 2 H) 4-744 Cl cyclobutylmethoxy SO₂Me 10.10 (bs, 1 H), 8.04 (d, 1 H), 7.61 (d, 1 H), 4.28 (d, 2 H), 4.14 (s, 3 H), 3.29 (s, 3 H), 2.94-2.97 (m, 1 H), 2.16-2.21 (m, 2 H), 1.95-2.03 (m, 4 H) 4-745 Cl cyclobutylmethoxy SO₂Et 9.88 (bs, 1 H), 8.02 (d, 1 H), 7.61 (d, 1 H), 4.29 (d, 2 H), 4.14 (s, 3 H), 3.45 (q, 2 H), 2.92-2.97 (m, 1 H), 2.14-2.20 (m, 2 H), 1.90-2.05 (m, 4 H), 1.27 (t, 3 H) 4-746 Cl 1,3-dioxolan-2- SO₂Me 8.05 (d, 1 H), 7.63 (d, 1 H), 5.50 ylmethoxy (t, 1 H), 4.31 (d, 2 H), 4.14 (s, 3 H), 4.07-4.10 (m, 2 H), 3.98- 4.01 (m, 2 H), 3.37 (s, 3 H) 4-747 Cl tetrahydro-2H-pyran- SO₂Me 10.20 (bs, 1 H), 8.04 (d, 1 H), 2-ylmethoxy 7.62 (d, 1 H), 4.41 (dd, 1 H), 4.14 (s, 3 H), 4.07-4.15 (m, 2 H), 3.89-3.94 (m, 1 H), 3.52-3.57 (m, 2 H), 3.35 (s, 3 H), 1.91-1.94 (m, 1 H), 1.55-1.70 (m, 4 H), 1.42-1.45 (m, 1 H) 4-748 Cl tetrahydrofuran-2H-pyran- SO₂Et 10.05 (bs, 1 H), 8.02 (d, 1 H), 2-ylmethoxy 7.62 (d, 1 H), 4.40 (dd, 1 H), 4.13 (s, 3 H), 4.07-4.13 (m, 2 H), 3.88-3.93 (m, 1 H), 3.47-3.59 (m, 3 H), 1.90-1.93 (m, 1 H), 1.55-1.68 (m, 4 H), 1.39-1.46 (m, 1 H), 1.23 (t, 3 H) 4-749 Cl tetrahydrofuran-3- SO₂Me 10.70 (bs, 1 H), 8.05 (d, 1 H), ylmethoxy 7.62 (d, 1 H), 4.28 (d, 2 H), 4.14 (s, 3 H), 3.91-3.98 (m, 2 H), 3.79-3.88 (m, 2 H), 3.29 (s, 3 H), 2.90-2.95 (m, 1 H), 2.12-2.18 (m, 1 H), 1.82-1.93 (m, 1 H) 4-750 Cl tetrahydrofuran-3- SO₂Et 10.60 (bs, 1 H), 8.03 (d, 1 H), ylmethoxy 7.62 (d, 1 H), 4.26 (d, 2 H), 4.14 (s, 3 H), 3.90-3.99 (m, 2 H), 3.79-3.86 (m, 2 H), 3.40-3.46 (m, 2 H), 2.88-2.95 (m, 1 H), 2.11-2.16 (m, 1 H), 1.80-1.89 (m, 1 H), 1.27 (t, 3 H) 4-751 Cl 3-(1H-tetrazol-1- SO₂Et 10.90 (bs, 1 H), 8.81 (s, 1 H), yl)propoxy 8.01 (d, 1 H), 7.63 (d, 1 H), 4.76 (t, 2 H), 4.35 (t, 2 H), 4.14 (s, 3 H), 3.35 (q, 2 H), 2.59 (quin, 2 H), 1.27 (t, 3 H) 4-752 Cl 3-(2H-tetrazol-2- SO₂Et 10.53 (bs, 1 H), 8.54 (s, 1 H), yl)propoxy 8.03 (d, 1 H), 7.63 (d, 1 H), 4.97 (t, 2 H), 4.38 (t, 2 H), 4.14 (s, 3 H), 3.42 (q, 2 H), 2.68 (quin, 2 H), 1.30 (t, 3 H) 4-753 Cl F SMe 7.71 (dd, 1 H), 7.23 (d, 1 H), 4.10 (s, 3 H), 2.55 (s, 3 H) 4-754 Cl F SOMe 7.90 (dd, 1 H), 7.81 (d, 1 H), 4.12 (s, 3 H), 2.92 (s, 3 H) 4-755 Cl F SO₂Me 3.25 (s, 3 H), 3.98 (s, 3 H), 7.68 (d, 1 H), 7.82 (d, 1 H), 8.60 (s, 1 H) 4-756 Cl SO₂Me SO₂Me 12.10 (s, 1 H), 8.40 (d, 1 H), 8.34 (d, 1 H), 4.03 (s, 3 H), 3.67 (s, 3 H), 3.58 (s, 3 H) 4-757 Cl SEt SO₂Me 8.23 (d, 1 H), 7.75 (d, 1 H), 4.15 (s, 3 H), 3.49 (s, 3 H), 3.08 (q, 2 H), 1.32 (t, 3 H) 4-758 Cl SOEt SO₂Me 8.15 (d, 1 H), 8.11 (d, 1 H), 4.01 (s, 3 H), 3.70 (m, 1 H), 3.54 (s, 3 H), 3.22 (m, 1 H), 1.36 (t, 3 H) 4-759 Cl SO₂Et SO₂Me 8.45 (d, 1 H), 7.96 (d, 1 H), 4.15 (s, 3 H), 3.72 (q, 2 H), 3.62 (s, 3 H), 1.55 (t, 3 H) 4-760 Cl S(CH₂)₂OMe SO₂Me 8.22 (d, 1 H), 7.75 (d, 1 H), 4.14 (s, 3 H), 3.66 (t, 2 H), 3.51 (s, 3 H), 3.32 (s, 3 H), 3.26 (t, 2 H) 4-761 Cl SO(CH₂)₂OMe SO₂Me 8.24 (d, 1 H), 7.88 (d, 1 H), 4.14 (s, 3 H), 4.01 (m, 2 H), 3.87 (m, 1 H), 3.54-3.39 (m, 1 H), 3.47 (s, 3 H), 3.44 (s, 3 H) 4-762 Cl SO₂(CH₂)₂OMe SO₂Me 8.45 (d, 1 H), 7.95 (d, 1 H), 4.15 (s, 3 H), 4.01 (t, 2 H), 3.96 (t, 2 H), 3.62 (s, 3 H), 3.33 (s, 3 H) 4-763 Br SMe Me 9.77 (bs, 1 H), 7.46 (d, 1 H), 7.34 (d, 1 H), 4.15 (s, 3 H), 2.69 (s, 3 H), 2.37 (s, 3 H) 4-764 Br SOMe Me 8.88 (bs, 1 H), 7.56 (d, 1 H), 7.31 (d, 1 H), 4.14 (s, 3 H), 2.98 (s, 3 H), 2.80 (s, 3 H) 4-765 Br SO₂Me Me 9.90 (bs, 1 H), 7.59 (d, 1 H), 7.45 (d, 1 H), 4.17 (s, 3 H), 3.34 (s, 3 H), 2.83 (s, 3 H) 4-766 Br SEt Me 9.30 (bs, 1 H), 7.46 (d, 1 H), 7.36 (d, 1 H), 4.15 (s, 3 H), 2.88 (q, 2 H), 2.68 (s, 3 H), 1.23 (t, 3 H) 4-767 Br SOEt Me 7.52-7.56 (m, 1 H), 7.30-7.36 (m, 1 H), 4.13 (s, 3 H), 3.21-3.26 (m, 1 H), 3.08-3.13 (m, 1 H), 2.70 (s, 3 H), 1.42 (t, 3 H) 4-768 Br SO₂Et Me 7.59 (d, 1 H), 7.45 (d, 1 H), 4.16 (s, 3 H), 3.49 (q, 2 H), 2.85 (s, 3 H), 1.37 (t, 3 H) 4-769 Br OEt Br 11.79 (bs, 1 H), 7.84 (d, 1 H), 7.41 (d, 1 H), 4.07 (q, 2 H), 4.01 (s, 3 H), 1.43 (t, 3 H) 4-770 Br O(CH₂)₃OMe Br 9.60 (bs, 1 H), 7.67 (d, 1 H), 7.31 (d, 1 H), 4.15 (t, 2 H), 4.13 (s, 3 H), 3.67 (t, 2 H), 3.39 (s, 3 H), 2.17 (quin, 2 H) 4-771 Br O(CH₂)₂SMe Br 11.82 (bs, 1 H), 7.85 (d, 1 H), 7.43 (d, 1 H), 4.16 (t, 2 H), 4.01 (s, 3 H), 2.97 (t, 2 H), 2.17 (s, 3 H) 4-772 Br O(CH₂)₃SMe Br 11.82 (bs, 1 H), 7.84 (d, 1 H), 7.42 (d, 1 H), 4.09 (t, 2 H), 4.01 (s, 3 H), 2.73 (t, 2 H), 2.09 (s, 3 H), 2.08 (quin, 2 H) 4-773 Br O(CH₂)₂SEt Br 11.82 (bs, 1 H), 7.85 (d, 1 H), 7.43 (d, 1 H), 4.14 (t, 2 H), 4.01 (s, 3 H), 3.00 (t, 2 H), 2.63 (q, 2 H), 1.22 (t, 3 H) 4-774 Br OCH₂(CO)NMe₂ Br 11.80 (bs, 1 H), 7.85 (d, 1 H), 7.45 (d, 1 H), 4.69 (s, 2 H), 4.01 (s, 3 H), 3.02 (s, 3 H), 2.88 (s, 3 H) 4-775 Br 1,4-dioxan-2- Br 11.85 (bs, 1 H), 7.82 (d, 1 H), ylmethoxy 7.40 (d, 1 H), 4.00-4.05 (m, 1 H), 4.00 (s, 3 H), 3.90-4.00 (m, 3 H), 3.77-3.80 (m, 1 H), 3.62- 3.70 (m, 2 H), 3.50-3.55 (m, 2 H) 4-776 Br tetrahydrofuran-2- Br 11.84 (bs, 1 H), 7.84 (d, 1 H), ylmethoxy 7.43 (d, 1 H), 4.25-4.30 (m, 1 H), 3.98-4.04 (m, 1 H), 4.00 (s, 3 H), 3.90 (dd, 1 H), 3.80-3.84 (m, 1 H), 3.69-3.72 (m, 1 H), 2.00-2.09 (m, 1 H), 1.84-1.89 (m, 3 H) 4-777 Br OMe I 11.80 (bs, 1 H), 8.00 (d, 1 H), 7.24 (d, 1 H), 4.01 (s, 3 H), 3.83 (s, 3 H) 4-778 Br OEt I 11.77 (bs, 1 H), 8.00 (d, 1 H), 7.22 (d, 1 H), 4.05 (q, 2 H), 4.01 (s, 3 H), 1.45 (t, 3 H) 4-779 Br O(CH₂)₂OMe I 10.20 (bs, 1 H), 7.92 (d, 1 H), 7.18 (d, 1 H), 4.23 (t, 2 H), 4.13 (s, 3 H), 3.89 (t, 2 H), 3.50 (s, 3 H) 4-780 Br O(CH₂)₃OMe I 10.00 (bs, 1 H), 7.91 (d, 1 H), 7.17 (d, 1 H), 4.13 (s, 3 H), 4.13 (t, 2 H), 3.68 (t, 2 H), 3.40 (s, 3 H), 2.19 (quin, 2 H) 4-781 Br O(CH₂)₂SMe I 11.80 (bs, 1 H), 8.01 (d, 1 H), 7.24 (d, 1 H), 4.13 (t, 2 H), 4.01 (s, 3 H), 2.99 (t, 2 H), 2.19 (s, 3 H) 4-782 Br O(CH₂)₂SEt I 11.80 (bs, 1 H), 8.00 (d, 1 H), 7.24 (d, 1 H), 4.11 (t, 2 H), 4.00 (s, 3 H), 3.02 (t, 2 H), 2.65 (q, 2 H), 1.23 (t, 3 H) 4-783 Br O(CH₂)₃SMe I 11.80 (bs, 1 H), 8.00 (d, 1 H), 7.23 (d, 1 H), 4.06 (t, 2 H), 4.00 (s, 3 H), 2.74 (t, 2 H), 2.11 (quin, 2 H), 2.09 (s, 3 H) 4-784 Br OCH₂(CO)NMe₂ I 11.82 (bs, 1 H), 8.00 (d, 1 H), 7.25 (d, 1 H), 4.65 (s, 3 H), 3.99 (s, 3 H), 3.02 (s, 3 H), 2.89 (s, 3 H) 4-785 Br 1,4-dioxan-2- I 11.80 (bs, 1 H), 8.00 (d, 1 H), ylmethoxy 7.23 (d, 1 H), 4.00-4.02 (m, 2 H), 3.99 (s, 3 H), 3.90-3.95 (m, 2 H), 3.79-3.81 (m, 1 H), 3.63- 3.72 (m, 2 H), 3.50-3.55 (m, 2 H) 4-786 Br tetrahydrofuran-2- I 11.79 (bs, 1 H), 8.00 (d, 1 H), ylmethoxy 7.23 (d, 1 H), 4.29-4.31 (m, 1 H), 4.00 (s, 3 H), 3.96-4.02 (m, 1 H), 3.80-3.90 (m, 2 H), 3.68- 3.75 (m, 1 H), 3.18 (s, 3 H), 2.02-2.07 (m, 1 H), 1.86-1.94 (m, 3 H) 4-787 Br OMe SMe 10.75 (bs, 1 H), 7.69 (d, 1 H), 7.59 (d, 1 H), 4.11 (s, 3 H), 3.98 (s, 3 H), 2.55 (s, 3 H) 4-788 Br OMe SO₂Me 7.93 (d, 1 H), 7.27 (d, 1 H), 4.21 (s, 3 H), 4.11 (s, 3 H), 3.32 (s, 3 H) 4-789 I SMe Me 9.96 (bs, 1 H), 7.37 (d, 1 H), 7.36 (d, 1 H), 4.20 (s, 3 H), 2.73 (s, 3 H), 2.34 (s, 3 H) 4-790 I SOMe Me 11.73 (bs, 1 H), 7.57 (d, 1 H), 7.48 (d, 1 H), 4.04 (s, 3 H), 2.94 (s, 3 H), 2.70 (s, 3 H) 4-791 I SO₂Me Me 4-792 I SEt Me 9.24 (bs, 1 H), 7.35 (d, 1 H), 7.31 (d, 1 H), 4.20 (s, 3 H), 2.86 (q, 2 H), 2.72 (s, 3 H), 1.26 (t, 3 H) 4-793 I SOEt Me 7.43 (d, 1 H), 7.31 (d, 1 H), 4.18 (s, 3 H), 3.14-3.21 (m, 1 H), 3.05-3.10 (m, 1 H), 2.68 (s, 3 H), 1.45 (t, 3 H) 4-794 I SO₂Et Me 9.65 (bs, 1 H), 7.47 (s, 2 H), 4.22 (s, 3 H), 3.42-3.49 (m, 2 H), 2.86 (s, 3 H), 1.40 (t, 3 H) 4-795 NO₂ SMe Me 11.72 (bs, 1 H), 8.11 (d, 1 H), 7.63 (d, 1 H), 4.05 (s, 3 H), 2.71 (s, 3 H), 2.36 (s, 3 H) 4-796 NO₂ SOMe Me 12.19 (bs, 1 H), 8.06 (d, 1 H), 7.77 (d, 1 H), 3.93 (s, 3 H), 3.14 (s, 3 H), 2.61 (s, 3 H) 4-797 NO₂ SO₂Me Me 12.21 (bs, 1 H), 8.22 (d, 1 H), 7.91 (d, 1 H), 3.93 (s, 3 H), 3.47 (s, 3 H), 2.79 (s, 3 H) 4-798 NO₂ SEt Me 11.41 (bs, 1 H), 8.06 (d, 1 H), 7.63 (d, 1 H), 4.05 (s, 3 H), 2.82 (q, 2 H), 2.70 (s, 3 H), 1.22 (t, 3 H) 4-799 NO₂ SOEt Me 12.14 (bs, 1 H), 8.06 (d, 1 H), 7.76 (d, 1 H), 3.93 (s, 3 H), 3.42- 3.51 (m, 1 H), 3.17-3.27 (m, 1 H), 2.61 (s, 3 H), 1.32 (t, 3 H) 4-800 NO₂ SO₂Et Me 12.12 (bs, 1 H), 8.00 (bs, 1 H), 7.62 (d, 1 H), 3.98 (s, 3 H), 3.46 (q, 2 H), 2.84 (s, 3 H), 1.48 (t, 3 H) 4-801 NO₂ CH₂OCH₂CF₃ Cl 3.78 (q, 2 H), 3.89 (s, 3 H), 4.72 (s, 2 H), 7.51 (d, 1 H), 8.18 (d, 1 H) 4-802 NO₂ NMe₂ Cl 2.77 (s, 6 H), 3.89 (s, 3 H), 7.39 (d, 1 H), 7.95 (s, br, 1 H) 4-803 OH SMe CHF₂ 8.31 (d, 1 H), 7.42 (m, 1 H), 7.21 (t, 1 H), 4.01 (s, 3 H), 2.39 (s, 3 H) 4-804 OH SOMe CHF₂ 8.45 (d, 1 H), 7.34 (d, 1 H), 6.80 (t, 1 H), 4.08 (s, 3 H), 3.17 (s, 3 H) 4-805 OH SO₂Me CHF₂ 8.24 (d, 1 H), 7.74 (t, 1 H), 7.10 (d, 1 H), 3.96 (s, 3 H), 3.42 (s, 3 H) 4-806 OH SMe CF₃ 8.09 (d, 1 H), 7.42 (d, 1 H), 3.98 (s, 3 H), 2.37 (s, 3 H) 4-807 OH SO₂Me CF₃ 8.10 (d, 1 H), 6.83 (d, 1 H), 3.94 (s, 3 H), 3.37 (s, 3 H) 4-808 OH SCH₂Ph CF₃ 7.92 (d, 1 H), 7.24-7.14 (m, 5 H), 6.82 (d, 1 H), 4.18 (s, 2 H), 3.87 (s, 3 H) 4-809 OMe SMe Me 4-810 OMe SOMe Me 4-811 OMe SO₂Me Me 4-812 OMe SMe CHF₂ 8.23 (d, 1 H), 7.66 (d, 1 H), 7.23 (t, 1 H), 4.19 (s, 3 H), 4.10 (s, 3 H), 2.47 (s, 3 H) 4-813 OMe SOMe CHF₂ 8.27 (d, 1 H), 7.93 (t, 1 H), 7.88 (d, 1 H), 4.12 (s, 6 H), 3.08 (s, 3 H) 4-814 OMe SO₂Me CHF₂ 8.33 (d, 1 H), 7.91 (d, 1 H), 7.83 (t, 1 H), 4.17 (s, 3 H), 4.14 (s, 3 H), 3.41 (s, 3 H) 4-815 OMe SMe OMe 8.15 (d, 1 H), 6.88 (d, 1 H), 4.12 (s, 3 H), 4.09 (s, 3 H), 4.01 (s, 3 H), 2.44 (s, 3 H) 4-816 OMe SOMe OMe 4-817 OMe SO₂Me OMe 8.37 (d, 1 H), 7.05 (d, 1 H), 4.17 (s, 3 H), 4.09 (s, 3 H), 4.08 (s, 3 H), 3.35 (s, 3 H) 4-818 OMe SMe F 8.12 (dd, 1 H), 7.09 (t, 1 H), 4.16 (s, 3 H), 4.08 (s, 3 H), 2.52 (s, 3 H) 4-819 OMe SOMe F 4-820 OMe SO₂Me F 4-821 OMe CH₂N(SO₂Me)Et Cl 11.51 (brs, 1 H), 7.70 (d, 1 H), 7.42 (d, 1 H), 4.52 (s, 2 H), 3.99 (s, 3 H), 3.87 (s, 3 H), 3.05 (q, 2 H), 3.01 (s, 3 H), 0.97 (t, 3 H) 4-822 OMe NHCOMe Cl 11.36 (brs, 1 H), 9.71 (brs, 1 H), 7.64 (d, 1 H), 7.45 (d, 1 H), 3.97 (s, 3 H), 3.81 (s, 3 H), 2.09 (s, 3 H) 4-823 OMe NHCOEt Cl 11.36 (brs, 1 H), 9.63 (brs, 1 H), 7.64 (d, 1 H), 7.45 (d, 1 H), 3.97 (s, 3 H), 3.80 (s, 3 H), 2.38 (q, 2 H), 1.13 (t, 3 H) 4-824 OMe NHCOiPr Cl 11.36 (brs, 1 H), 9.59 (brs, 1 H), 7.65 (d, 1 H), 7.45 (d, 1 H), 3.97 (s, 3 H), 3.79 (s, 3 H), 2.70 (m, 1 H), 1.15 (d, 6 H) 4-825 OMe NHCOcPr Cl 11.36 (brs, 1 H), 9.81 (brs, 1 H), 7.64 (d, 1 H), 7.45 (d, 1 H), 3.98 (s, 3 H), 3.84 (s, 3 H) 4-826 OMe NHCOCHCMe₂ Cl 11.35 (brs, 1 H), 9.56 (brs, 1 H), 7.64 (d, 1 H), 7.45 (d, 1 H), 5.97 (s, 1 H), 3.97 (s, 3 H), 3.79 (s, 3 H), 2.13 (s, 3 H), 1.18 (s, 3 H) 4-827 OMe NHCOPh Cl 11.42 (brs, 1 H), 10.19 (brs, 1 H), 8.03 (d, 2 H), 7.72 (d, 1 H), 7.63 (m, 1 H), 7.57 (t, 2 H), 7.53 (d, 1 H), 3.97 (s, 3 H), 3.80 (s, 3 H), 2.38 (q, 2 H), 1.13 (t, 3 H) 4-828 OMe SO₂Me SO₂Me 4-829 OEt SMe CF₃ 4-830 OEt SOMe CF₃ 4-831 OEt SO₂Me CF₃ 4-832 OEt SEt CF₃ 4-833 OEt SOEt CF₃ 4-834 OEt SO₂Et CF₃ 4-835 OEt S(CH₂)₂OMe CF₃ 4-836 OEt SO(CH₂)₂OMe CF₃ 4-837 OEt SO(CH₂)₂OMe CF₃ 4-838 OEt SMe Cl 1.62 (t, 2 H), 2.48 (s, 3 H), 4.09 (s, 3 H), 4.37 (q, 2 H), 7.43 (d, 1 H), 8.03 (d, 1 H), 10.58 (s, 1 H) 4-839 OEt SOMe Cl 4-840 OEt SO₂Me Cl 4-841 OEt SEt Cl 4-842 OEt SOEt Cl 4-843 OEt SO₂Et Cl 4-844 OEt S(CH₂)₂OMe Cl 4-845 OEt SO(CH₂)₂OMe Cl 4-846 OEt SO(CH₂)₂OMe Cl 8-847 OSO₂Me SMe CF₃ 7.97 (s, 2 H), 4.02 (s, 3 H), 3.63 (s, 3 H), 2.51 (s, 3 H) 8-848 OSO₂Me SOMe CF₃ 8-849 OSO₂Me SO₂Me CF₃ 8.30 (d, 1 H), 8.22 (d, 1 H), 4.03 (s, 3 H), 3.66 (s, 3 H), 3.57 (s, 3 H) 8-850 OSO₂Et SMe CF₃ 12.01 (brs, 1 H), 7.98 (brs, 2 H), 4.02 (s, 3 H), 3.77 (q, 2 H), 2.51 (s, 3 H), 1.42 (t, 3 H) 8-851 OSO₂Et SOMe CF₃ 8-852 OSO₂Et SO₂Me CF₃ 8-853 OSO₂CF₃ SMe CF₃ 12.29 (brs, 1 H), 8.19 (d, 1 H), 8.16 (d, 1 H), 4.00 (s, 3 H), 3.63 (s, 3 H), 2.51 (s, 3 H) 8-854 OSO₂CF₃ SOMe CF₃ 8-855 OSO₂CF₃ SO₂Me CF₃ 8-856 SMe SMe H 7.54 (t, 1 H), 7.39 (d, 1 H), 7.36 (d, 1 H), 4.04 (s, 3 H), 2.49 (s, 3 H), 2.35 (s, 3 H) 8-857 SO₂Me SO₂Me H 12.02 (brs, 1 H), 8.40 (d, 1 H), 8.20-8.14 (m, 2 H), 4.04 (s, 3 H), 3.58 (s, 6 H) 8-858 SO₂Me SO₂Me Me 8-859 SO₂Me NMe₂ CF₃ 8-860 SO₂Me NHMe CF₃ 8-861 SO₂Me pyrazol-1-yl CF₃ 4-862 SMe OMe F 11.60 (s, 1 H), 7.39-7.46 (m, 2 H), 4.02 (s, 3 H), 3.96 (d, 3 H), 2.43 (s, 3 H) 4-863 SO₂Me OMe F 10.89 (bs, 1 H), 7.47 (t, 1 H), 7.35 (bs, 1 H), 4.20 (s, 3 H), 4.12 (s, 3 H), 3.27 (s, 3 H) 4-864 SO₂Me NMe₂ Cl 7.66 (d, 1 H), 7.39 (d, 1 H), 4.19 (s, 3 H), 3.35 (s, 3 H), 2.94 (s, 6 H) 4-865 SO₂Me NHMe Cl 4-866 SO₂Me NH₂ Cl 7.58 (d, 1 H), 6.92 (d, 1 H), 6.05 (brs, 2 H), 4.17 (s, 3 H), 3.29 (s, 3 H) 4-867 SO₂Me NHcHex Cl 7.55 (d, 1 H), 7.00 (d, 1 H), 6.27 (brd, 1 H), 4.16 (s, 3 H), 3.92 (m, 1 H), 3.31 (s, 3 H), 2.03 (m, 2 H), 1.78 (m, 2 H), 1.68- 1.53 (m, 2 H), 1.38-1.12 (m, 4 H) 4-868 SMe OCH2CHF2 Br 11.68 (s, 1 H), 7.83 (d, 1 H), 7.39 (d, 1 H), 6.48 (tt, 1 H), 4.38 (dt, 2 H), 4.02 (s, 3 H), 2.44 (s, 3 H) 4-869 SO₂Me OMe SO₂Me 4-870 SMe O(CH₂)₂OMe SMe 11.53 (s, 1 H), 7.38 (d, 1 H), 7.28 (d, 1 H), 4.09 (t, 2 H), 4.01 (s, 3 H), 3.56 (t, 2 H), 3.26 (s, 3 H), 2.46 (s, 3 H), 2.40 (s, 3 H), 2.03 (quin, 2 H) 4-871 SO₂Me F SO₂Me 4-872 SO₂Me SMe SO₂Me 4-873 SO₂Me SO₂Me SO₂Me 4-874 Me NH(CH₂)₂OMe SO₂Me 2.45 (s, 3 H), 3.19 (s, 3 H), 3.39 (s, 3 H), 3.42 (t, 2 H), 3.60 (t, 2 H), 4.11 (s, 3 H), 5.82 (br, s, 1 H), 7.26 (d, 1 H), 7.77 (d, 1 H), 10.57 (s, 1 H) 4-875 CF₃ 2-(1H-pyrazol-1- SO₂Me 8.05-8.15 (bs, 1 H), 7.68 (d, yl)ethoxy 1 H), 7.57 (d, 1 H), 7.46 (d, 1 H), 6.46 (t, 1 H), 4.51-4.57 (m, 4 H), 3.76-3.87 (m, 3 H), 3.03 (s, 3 H) 4-876 CF₃ SMe SO₂Me 12.01 (s, 1 H), 8.49 (d, 1 H), 8.15 (d, 1 H), 4.01 (s, 3 H), 3.63 (s, 3 H), 2.53 (s, 3 H) 4-877 CF₃ tetrahydrofuran-2- SO₂Et ylmethoxy 4-878 CF₃ tetrahydrofuran-2- SO₂Me ylmethoxy 4-879 CF₃ OEt SO₂Me 12.04 (s, 1 H), 8.30 (d, 1 H), 7.87 (d, 1 H), 4.26 (q, 2 H), 3.99 (s, 3 H), 3.42 (s, 3 H), 1.45 (t, 3 H) 4-880 CF₃ SMe SO₂Et 4-881 Cl 5-methoxymethyl- SO₂Et 1.26 (t, 3 H), 3.23 (dd, 1 H), 3.37 4,5-dihydro-1,2- (q, 2 H), 3.45 (s, 3 H), 3.48 oxazol-3-yl (dd, 1 H), 3.58 (dd, 1 H), 3.71 (dd, 1 H), 4.11 (s, 3 H), 5.05 (m, 1 H), 7.88 (d, 1 H), 8.05 (d, 1 H), 10.8 (br, s, 1 H) 4-882 Cl 5-methoxymethyl-5- SO₂Et 1.26 (t, 3 H), 1.53 (s, 3 H), 3.09 methyl-4,5-dihydro- (d, 1 H), 3.41 (q, 2 H), 3.45 1,2-oxazol-3-yl (s, 3 H), 3.45 (d, 1 H), 3.53 (q, 2 H), 4.11 (s, 3 H), 7.85 (d, 1 H), 7.98 (d, 1 H), 10.8 (br, s, 1 H) 4-883 CF₃ SO₂Me SO₂Et 8.44 (d, 1 H), 8.08 (d, 1 H), 3.98 (s, 3 H), 3.51-3.55 (m, 2 H), 3.27 (s, 3 H), 1.22 (t, 3 H) 4-884 CF₃ SOMe SO₂Et 8.62 (d, 1 H), 8.28 (d, 1 H), 4.07 (s, 3 H), 3.83 (q, 2 H), 3.72 (s, 3 H), 1.42 (t, 3 H) 4-885 Cl 2,4-dichloro-thiazol- SO₂Et 5-yloxy 4-886 Me SEt Br 10.08 (bs, 1 H), 7.71 (d, 1 H), 7.52 (d, 1 H), 4.11 (s, 3 H), 2.89 (q, 2 H), 2.81 (s, 3 H), 1.23 (t, 3 H) 4-887 Me SEt I 9.88 (bs, 1 H), 7.99 (d, 1 H), 7.31 (d, 1 H), 4.11 (s, 3 H), 2.86 (q, 2 H), 2.85 (s, 3 H), 1.26 (t, 3 H) 4-888 SMe 4-MeO-benzyloxy Br 11.69 (s, 1 H), 7.82 (d, 1 H), 7.52 (d, 2 H), 7.37 (d, 1 H), 7.00 (d, 2 H), 5.01 (s, 2 H), 4.03 (s, 3 H), 3.79 (s, 3 H), 2.43 (s, 3 H) 4-889 Me NHCH₂CH₂OCOiPr SO₂Me 1.20 (d, 6 H), 2.49 (s, 3 H), 2.61 (m, 1 H), 3.13 (s, 3 H), 3.51 (m, 2 H), 4.11 (s, 3 H), 4.31 (m, 2 H), 4.11 (s, 3 H), 4.31 (m, 2 H), 5.82 (t, 1 H), 7.34 (d, 1 H), 7.84 (d, 1 H), 11.01 (s, 1 H) 4-890 Me NHCH₂CH₂OCOcPr SO₂Me 0.91 (m, 2 H), 1.04 (m, 2 H), 1.62 (m, 1 H), 2.49 (s, 3 H), 3.15 (s, 3 H), 3.51 (m, 2 H), 4.12 (s, 3 H), 4.31 (m, 2 H), 5.83 (t, 1 H), 7.33 (d, 1 H), 7.84 (d, 1 H), 10.82 (s, 1 H) 4-891 CF₃ O(CH₂)₃OMe SO₂Me 12.04 (s, 1 H), 8.30 (d, 1 H), 7.86 (d, 1 H), 4.27 (t, 2 H), 3.97 (s, 3 H), 3.52 (t, 2 H), 3.42 (s, 3 H), 3.27 (s, 3 H), 2.08 (quin, 2 H) 4-892 Me NH(CH₂)₃OEt SO₂Me 1.21 (t, 3 H), 1.94 (m, 2 H), 2.47 (s, 3 H), 3.13 (s, 3 H), 3.32 (t, 2 H), 3.51 (q, 2 H), 3.58 (t, 2 H), 4.12 (s, 3 H), 5.63 (br, s, 1 H), 7.29 (d, 1 H), 7.80 (d, 1 H), 10.73 (s, 1 H) 4-893 CH₂SMe H CF₃ 4-894 CH₂SMe H Br 11.67 (bs, 1 H), 7.71 s, 1 H), 7.71-7.67 (m, 2 H), 3.99 (s, 3 H), 3.95 (s, 2 H), 1.95 (s, 3 H) 4-895 F SMe Cl 2.55 (s, 3 H), 4.06 (s, 3 H), 7.44 (d, 1 H), 7.93 (t, 1 H), 9.92 (s, 1 H) 4-896 Me F SO₂Me 2.51 (s, 3 H), 3.27 (s, 3 H), 4.12 (s, 3 H), 7.72 (d, 1 H), 7.94 (d, 1 H), 10.4 (s, 1 H) 4-897 Cl NH₂ SO₂Me 3.04 (s, 3 H), 3.97 (s, 3 H), 6.94 (d, 1 H), 7.69 (d, 1 H) 4-898 F SOMe Cl 3.21 (s, 3 H), 4.06 (s, 3 H), 7.43 (d, 1 H), 8.09 (t, 1 H), 10.21 (s, 1 H) 4-899 F SO₂Me Cl 4-900 CH₂SO₂Me H Br 11.67 (brs, 1 H), 7.71 (d, 1 H), 7.69 (d, 1 H), 7.66 (dd, 1 H), 3.99 (s, 3 H), 3.95 (s, 2 H), 1.95 (s, 3 H) 4-901 Br 1,4-dioxan-2- SO₂Me ylmethoxy 4-902 Me OCH₂CONEt₂ Br 4-903 Cl 4,6-dimethoxy- Cl 11.90 (bs, 1 H), 7.67 (d, 1 H), pyrimidin-2- 7.54 (d, 1 H), 6.24 (s, 1 H), 4.09 ylmethoxy (s, 2 H), 3.98 (s, 3 H), 3.84 (s, 6 H) 4-904 Me SOMe imidazol-1-yl 4-905 Et 1,4-dioxan-2- SO₂Me ylmethoxy 4-906 F SO₂CH₂Ph CF₃ 4-907 SO₂Me OCH2CHF2 Br 7.96 (bs, 1 H), 7.20 (bs, 1 H), 6.51 (t, 1 H), 4.49 (t, 2 H), 4.00 (s, 3 H), 3.40 (s, 3 H) 4-908 Me COOMe SO₂Me 4-909 Cl CH₂(4-cyclopropyl-3- Cl (methylsulfanyl)-5- oxo-4,5-dihydro-1H- 1,2,4-triazol-1-yl) 4-910 Cl Me SO₂Me 4-911 Cl 2-(1H-tetrazol-1- SO₂Et 11.05 (bs, 1 H), 8.88 (s, 1 H), yl)ethoxy) 8.01 (d, 1 H), 7.64 (d, 1 H), 4.98 (t, 2 H), 4.77 (t, 2 H), 4.14 (s, 3 H), 3.22 (q, 2 H), 1.25 (t, 3 H) 4-912 Cl 2-(2H-tetrazol-2- SO₂Et 10.90 (bs, 1 H), 8.60 (s, 1 H), yl)ethoxy 8.01 (d, 1 H), 7.63 (d, 1 H), 5.19 (t, 2 H), 4.81 (t, 2 H), 4.12 (s, 3 H), 3.36 (q, 2 H), 1.26 (t, 3 H) 4-913 Cl OCH₂CH₂Cl SO₂Me 10.58 (bs, 1 H), 8.06 (d, 1 H), 7.65 (d, 1 H), 4.58 (t, 2 H), 4.14 (s, 3 H), 3.98 (t, 2 H), 3.35 (s, 3 H) 4-914 Cl OCH₂CH₂Cl SO₂Et 10.86 (bs, 1 H), 8.04 (d, 1 H), 7.64 (d, 1 H), 4.56 (t, 2 H), 4.14 (s, 3 H), 3.97 (t, 2 H), 3.51 (q, 2 H), 1.30 (t, 3 H) 4-915 Me OEt CF₃ 10.24 (bs, 1 H), 7.62 (d, 1 H), 7.58 (d, 1 H), 4.11 (s, 3 H), 3.99 (q, 2 H), 2.50 (s, 3 H), 1.48 (t, 3 H) 4-916 CF₃ SO₂Me SO₂Me 4-917 F SOCH₂Ph CF₃ 4-918 Cl SCH₂c-Pr Cl 7.61 (d, 1 H), 7.56 (d, 1 H), 4.12 (s, 3 H), 2.87 (d, 2 H), 1.00 (m, 1 H), 0.52 (m, 2 H), 0.16 (m, 2 H) 4-919 Cl SOCH₂c-Pr Cl 7.68 (d, 1 H), 7.48 (d, 1 H), 4.10 (s, 3 H), 3.44 (m, 1 H), 3.14 (m, 1 H), 1.02 (m, 1 H), 0.74 (m, 1 H), 0.66 (m, 1 H), 0.44 (m, 1 H), 0.25 (m, 1 H) 4-920 Cl SO₂CH₂c-Pr Cl 8.03 (d, 1 H), 7.88 (d, 1 H), 4.02 (s, 3 H), 3.57 (d, 2 H), 1.01 (m, 1 H), 0.53 (m, 2 H), 0.24 (m, 2 H) 4-921 F SEt CF₃ 8.12 (dd, 1 H), 7.71 (d, 1 H), 4.09 (s, 3 H), 3.02 (q, 2 H), 1.27 (t, 3 H) 4-922 F SOEt CF₃ 8.25 (dd, 1 H), 7.74 (d, 1 H), 4.07 (s, 3 H), 3.61 (m, 1 H), 3.29 (m, 1 H), 1.41 (t, 3 H) 4-923 F SO₂Et CF₃ 8.31 (dd, 1 H), 7.91 (d, 1 H), 4.09 (s, 3 H), 3.62 (q, 2 H), 1.47 (t, 3 H) 4-924 F SEt Cl 7.97 (dd, 1 H), 7.47 (dd, 1 H), 4.07 (s, 3 H), 3.01 (q, 2 H), 1.27 (t, 3 H) 4-925 F SOEt Cl 8.05 (dd, 1 H), 7.41 (d, 1 H), 4.05 (s, 3 H), 3.51 (m, 1 H), 3.39 (m, 1 H), 1.39 (t, 3 H) 4-926 F SO₂Et Cl 8.10 (dd, 1 H), 7.75 (d, 1 H), 3.98 (s, 3 H), 3.57 (q, 2 H), 1.25 (t, 3 H) 4-927 Me I SO₂Me 8.03 (d, 1 H), 7.80 (d, 1 H), 3.95 (s, 3 H), 3.43 (s, 3 H), 2.60 (s, 3 H) 4-928 Me I SMe 4-929 Me CN SO₂Me 4-930 Me CF₃ SO₂Me 4-931 Me pyrazol-1-yl SMe 4-932 Me 1,2,4-triazol-4-yl SO₂Me 4-933 Me COOMe SMe 4-934 Me COOMe SO₂Me

TABLE 5 Compounds of the formula (I) according to the invention in which A represents CY, B represents N and R represents ethyl.

Physical data No. X Y Z (¹H—NMR, DMSO-d₆, 400 MHz) 5-1 F H Cl 5-2 F H Br 5-3 F H SO₂Me 5-4 F H SO₂Et 5-5 F H CF₃ 5-6 F H NO₂ 5-7 Cl H F 5-8 Cl H Cl 11.71 (brs, 1H), 7.82 (d, 1H), 7.78 (d, 1H), 7.62 (dd, 1H), 4.35 (q, 2H), 1.47 (t, 3H) 5-9 Cl H Br 5-10 Cl H SMe 5-11 Cl H SOMe 5-12 Cl H SO₂Me 5-13 Cl H SO₂CH₂Cl 5-14 Cl H SEt 5-15 Cl H SO₂Et 11.87 (brs, 1H), 8.12 (s, 1H), 8.04 (d, 1H), 8.01 (d, 1H), 4.38 (q, 2H), 3.47 (q, 2H), 1.48 (t, 3H), 1.14 (t, 3H) 5-16 Cl H CF₃ 5-17 Cl H NO₂ 5-18 Cl H pyrazol-1-yl 5-19 Cl H 1H-1,2,4-triazol- 11.76 (brs, 1H), 9.48 (s, 1H), 8.33 1-yl (s, 1H), 8.19 (d, 1H), 8.03 (dd, 1H), 7.95 (d, 1H), 4.37 (q, 2H), 1.48 (t, 3H) 5-20 Br H Cl 5-21 Br H Br 11.92 (brs, 1H), 7.80 (d, 2H), 7.41 (t, 1H), 4.43 (q, 2H), 1.49 (t, 3H) 5-22 Br H SO₂Me 5-23 Br H SO₂Et 5-24 Br H CF₃ 8.20 (s, 1H), 7.94 (s, 2H), 4.39 (q, 2H), 1.49 (t, 3H) 5-25 SO₂Me H Cl 8.04 (s, 1H), 8.02 (d, 1H), 7.93 (d, 1H), 4.39 (q, 2H), 3.42 (s, 3H), 1.44 (t, 3H) 5-26 SO₂Me H Br 8.16 (s, 1H), 8.15 (d, 1H), 7.88 (d, 1H), 4.38 (q, 2H), 3.41 (s, 3H), 1.43 (t, 3H) 5-27 SO₂Me H SMe 5-28 SO₂Me H SOMe 5-29 SO₂Me H SO₂Me 5-30 SO₂Me H SO₂Et 5-31 SO₂Me H CF₃ 8.34 (d, 1H), 8.31 (s, 1H), 8.16 (d, 1H), 4.42 (q, 2H), 3.45 (s, 3H), 1.47 (t, 3H) 5-32 SO₂Et H Cl 5-33 SO₂Et H Br 5-34 SO₂Et H SMe 5-35 SO₂Et H SOMe 5-36 SO₂Et H SO₂Me 5-37 SO₂Et H CF₃ 5-38 NO₂ H F 5-39 NO₂ H Cl 5-40 NO₂ H Br 11.93 (brs, 1H), 8.44 (d, 1H), 8.17 (dd, 1H), 7.87 (d, 1H), 4.36 (q, 2H), 1.47 (t, 3H) 5-41 NO₂ H I 11.90 (brs, 1H), 8.53 (d, 1H), 8.31 (dd, 1H), 7.68 (d, 1H), 4.35 (q, 2H), 1.47 (t, 3H) 5-42 NO₂ H CN 12.05 (brs, 1H), 8.82 (d, 1H), 8.44 (d, 1H), 8.15 (brs, 1H), 4.38 (q, 2H), 1.48 (t, 3H) 5-43 NO₂ H SO₂Me 5-44 NO₂ H SO₂Et 5-45 NO₂ H CF₃ 5-46 Me H Cl 5-47 Me H Br 5-48 Me H SMe 5-49 Me H SO₂Me 5-50 Me H SO₂CH₂Cl 5-51 Me H SEt 5-52 Me H SO₂Et 5-53 Me H CF₃ 5-54 CH₂SO₂Me H CF₃ 5-55 Et H Cl 11.48 (brs, 1H), 7.67 (d, 1H), 7.49 (d, 1H), 7.44 (dd, 1H), 4.32 (q, 2H), 2.78 (q, 2H), 1.46 (t, 3H), 1.18 (t, 3H) 5-56 Et H Br 7.63 (s, 1H), 7.58 (2s, 2H), 4.32 (q, 2H), 2.77 (q, 2H), 1.46 (t, 3H), 1.18 (t, 3H) 5-57 Et H SMe 5-58 Et H SO₂Me 5-59 Et H SO₂CH₂Cl 5-60 Et H SEt 5-61 Et H SO₂Et 5-62 Et H CF₃ 5-63 CF₃ H Cl 11.81 (brs, 1H), 8.03 (s, 1H), 7.98- 7.79 (m, 2H), 4.33 (q, 2H), 1.46 (t, 3H) 5-64 CF₃ H Br 5-65 CF₃ H SO₂Me 5-66 CF₃ H SO₂Et 5-67 CF₃ H CF₃ 7.89 (s, 1H), 7.75 (d, 1H), 7.68 (d, 1H), 4.31 (q, 2H), 1.49 (t, 3H) 5-68 NO₂ NH₂ F 5-69 NO₂ NHMe F 5-70 NO₂ NMe₂ F 5-71 NO₂ Me Cl 5-72 NO₂ NH₂ Cl 5-73 NO₂ NHMe Cl 5-74 NO₂ NMe₂ Cl 5-75 NO₂ NH₂ Br 5-76 NO₂ NHMe Br 5-77 NO₂ NMe₂ Br 5-78 NO₂ NH₂ CF₃ 5-79 NO₂ NMe₂ CF₃ 5-80 NO₂ NH₂ SO₂Me 5-81 NO₂ NH₂ SO₂Et 5-82 NO₂ NHMe SO₂Me 5-83 NO₂ NMe₂ SO₂Me 5-84 NO₂ NMe₂ SO₂Et 5-85 NO₂ NH₂ 1H-1,2,4-triazol- 1-yl 5-86 NO₂ NHMe 1H-1,2,4-triazol- 1-yl 5-87 NO₂ NMe₂ 1H-1,2,4-triazol- 1-yl 5-88 Me SMe H 5-89 Me SOMe H 5-90 Me SO₂Me H 5-91 Me SEt H 5-92 Me SOEt H 5-93 Me SO₂Et H 5-94 Me S(CH₂)₂OMe H 5-95 Me SO(CH₂)₂OMe H 5-96 Me SO₂(CH₂)₂OMe H 5-97 Me F F 5-98 Me F Cl 5-99 Me SEt F 5-100 Me SOEt F 5-101 Me SO₂Et F 5-102 Me Me Cl 7.37 (d, 1H), 7.17 (d, 1H), 4.34 (q, 2H), 2.31 (s, 3H), 2.30 (s, 3H), 1.46 (t, 3H) 5-103 Me F Cl 5-104 Me Cl Cl 5-105 Me NH₂ Cl 5-106 Me NHMe Cl 5-107 Me NMe₂ Cl 5-108 Me O(CH₂)₂OMe Cl 11.47 (brs, 1H), 7.50 (d, 1H), 7.43 (d, 1H), 4.32 (q, 2H), 4.05 (m, 2H), 3.68 (m, 2H), 3.30 (s, 3H), 2.38 (s, 3H), 1.46 (t, 3H) 5-109 Me O(CH₂)₃OMe Cl 11.49 (bs, 1H), 7.50 (d, 1H), 7.43 (d, 1H), 4.31 (q, 2H), 3.94 (t, 2H), 3.56 (t, 2H), 3.27 (s, 3H), 2.36 (s, 3H), 2.01 (quin, 2H), 1.46 (t, 3H) 5-110 Me O(CH₂)₄OMe Cl 5-111 Me OCH₂CONMe₂ Cl 11.47 (bs, 1H), 7.51 (d, 1H), 7.45 (d, 1H), 4.65 (s, 2H), 4.32 (q, 2H), 2.99 (s, 3H), 2.88 (s, 3H), 2.33 (s, 3H), 1.47 (t, 3H) 5-112 Me O(CH₂)₂—CO—NMe₂ Cl 5-113 Me O(CH₂)₂—NH(CO)NMe₂ Cl 5-114 Me O(CH₂)₂—NH(CO)NHCO₂Et Cl 5-115 Me O(CH₂)₂—NHCO₂Me Cl 5-116 Me O—CH₂—NHSO₂cPr Cl 5-117 Me O(CH₂)-5-2,4- Cl dimethy1-2,4-dihydro- 3H-1,2,4-triazol-3- one 5-118 Me O(CH₂)-3,5-dimethyl- Cl 1,2-oxazol-4-y1 5-119 Me SMe Cl 7.61 (d, 1H), 7.50 (d, 1H), 4.47 (q, 2H), 2.79 (s, 3H), 2.39 (s, 3H), 1.63 (t, 3H) 5-120 Me SOMe Cl 7.75 (d, 1H), 7.59 (d, 1H), 4.35 (q, 2H), 3.04 (s, 3H), 2.73 (s, 3H), 1.47 (t, 3H) 5-121 Me SO₂Me Cl 7.86 (d, 1H), 7.73 (d, 1H), 4.35 (q, 2H), 3.46 (s, 3H), 2.72 (s, 3H), 1.47 (t, 3H) 5-122 Me SEt Cl 7.55 (m, 1H), 7.45 (m, 1H), 4.45 (q, 2H), 2.87 (q, 2H), 2.75 (s, 3H), 1.61 (t, 3H) 5-123 Me SOEt Cl 7.63 (d, 1H), 7.39 (d, 1H), 4.44 (q, 2H), 3.31 (m, 1H), 3.11 (m, 1H), 2.73 (s, 3H), 1.62 (t, 3H), 1.35 (t, 3H) 5-124 Me SO₂Et Cl 7.69 (d, 1H), 7.56 (d, 1H), 4.48 (q, 2H), 3.48 (q, 2H), 2.84 (s, 3H), 1.63 (t, 3H), 1.37 (t, 3H) 5-125 Me S(CH₂)₂OMe Cl 5-126 Me SO(CH₂)₂OMe Cl 5-127 Me SO₂(CH₂)₂OMe Cl 5-128 Me NH₂ Br 5-129 Me NHMe Br 5-130 Me NMe₂ Br 5-131 Me OCH₂(CO)NMe₂ Br 11.47 (bs, 1H), 7.64 (d, 1H), 7.38 (d, 1H), 4.62 (s, 2H), 4.32 (q, 2H), 2.99 (s, 3H), 2.88 (s, 3H), 2.38 (s, 3H), 1.46 (t, 3H) 5-132 Me O(CH₂)-5-pyrrolidin- Br 2-one 5-133 Me SMe Br 5-134 Me SOMe Br 5-135 Me SO₂Me Br 5-136 Me SEt Br 9.78 (bs, 1H), 7.68 (d, 1H), 7.49 (d, 1H), 4.47 (q, 2H), 2.88 (q, 2H), 2.81 (s, 3H), 1.63 (t, 3H), 1.23 (t, 3H) 5-137 Me SOEt Br 5-138 Me SO₂Et Br 5-139 Me SMe I 9.94 (bs, 1H), 7.98 (d, 1H), 7.31 (d, 1H), 4.46 (q, 2H), 2.87 (s, 3H), 2.36 (s, 3H), 1.63 (t, 3H) 5-140 Me SOMe I 11.20 (bs, 1H), 7.91 (d, 1H), 7.35 (d, 1H), 4.45 (q, 2H), 2.91 (s, 3H), 2.76 (s, 3H), 2.17 (s, 3H), 1.62 (t, 3H) 5-141 Me SO₂Me I 11.72 (bs, 1H), 7.66 (d, 1H), 7.59 (d, 1H), 4.44 (q, 2H), 3.40 (s, 3H), 2.76 (s, 3H), 1.49 (t, 3H) 5-142 Me SEt I 10.17 (bs, 1H), 8.00 (d, 1H), 7.33 (d, 1H), 4.46 (q, 2H), 2.86 (q, 2H), 2.85 (s, 3H), 1.63 (t, 3H), 1.25 (t, 3H) 5-143 Me SOEt 5-144 Me SO₂Et I 9.76 (bs, 1H), 8.24 (d, 1H), 7.32 (d, 1H), 4.47 (q, 2H), 3.44 (q, 2H), 2.87 (s, 3H), 1.64 (t, 3H), 1.41 (t, 3H) 5-145 Me Cl CF₃ 7.45 (d, 1H), 7.32 (d, 1H), 4.29 (q, 2H), 2.39 (s, 3H), 1.48 (t, 3H) 5-146 Me SMe CF₃ 7.82 (d, 1H), 7.80 (d, 1H), 4.36 (q, 2H), 2.71 (s, 3H), 2.32 (s, 3H), 1.48 (t, 3H) 5-147 Me SOMe CF₃ 7.97 (d, 1H), 7.90 (d, 1H), 4.37 (q, 2H), 3.05 (s, 3H), 2.88 (s, 3H), 1.48 (t, 3H) 5-148 Me SO₂Me CF₃ 7.71 (d, 1H), 7.67 (d, 1H), 4.31 (q, 2H), 3.20 (s, 3H), 2.64 (s, 3H), 1.49 (t, 3H) 5-149 Me SEt CF₃ 7.76 (s, 2H), 4.48 (q, 2H), 2.82 (s, 3H), 2.79 (q, 2H), 1.64 (t, 3H), 1.23 (t, 3H) 5-150 Me SOEt CF₃ 7.76 (d, 1H), 7.71 (d, 1H), 4.48 (q, 2H), 3.44 (dd, 1H), 3.01-2.91 (m, 1H), 2.92 (s, 3H), 1.64 (t, 3H), 1.40 (t, 3H) 5-151 Me SO₂Et CF₃ 7.93 (d, 1H), 7.88 (d, 1H), 4.48 (q, 2H), 3.35 (q, 2H), 2.84 (s, 3H), 1.64 (t, 3H), 1.49 (t, 3H) 5-152 Me S(CH₂)₂OMe CF₃ 5-153 Me SO(CH₂)₂OMe CF₃ 5-154 Me SO₂(CH₂)₂OMe CF₃ 5-155 Me Me SO₂Me 5-156 Me 4,5-dihydro-1,2- SO₂Me 8.12 (d, 1H), 7.91 (d, 1H), 4.60 (t, 2H), oxazol-3-yl 4.45 (q, 2H), 3.38 (m, 2H), 3.20 (s, 3H), 2.48 (s, 3H), 1.62 (t, 3H) 5-157 Me 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 5-158 Me 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol-3- yl 5-159 Me 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol-3- yl 5-160 Me NH₂ SO₂Me 11.52 (brs, 1H), 7.59 (d, 1H), 6.93 (d, 1H), 6.09 (brs, 2H), 4.33 (q, 2H), 3.17 (s, 3H), 2.21 (s, 3H), 1.47 (t, 3H) 5-161 Me NHMe SO₂Me 5-162 Me NMe₂ SO₂Me 5-163 Me NH(CH₂)₂OMe SO₂Me 1.62 (t, 3H), 2.45 (s, 3H), 3.19 (s, 3H), 3.39 (s, 3H), 3.42 (m, 2H), 3.60 (m, 2H), 4.46 (q, 2H), 5.82 (s, br, 1H), 7.25 (d, 1H), 7.77 (d, 1H), 10.64 (s, 1H) 5-164 Me pyrrazol-1-yl SO₂Me 8.11 (d, 1H), 8.07 (d, 1H), 7.99 (d, 1H), 7.87 (d, 1H), 6.59 (dd, 1H), 4.36 (q, 2H), 3.04 (s, 3H), 1.92 (s, 3H), 1.47 (t, 3H) 5-165 Me OH SO₂Me 5-166 Me OMe SO₂Me 11.63 (bs, 1H), 7.82 (d, 1H), 7.63 (d, 1H), 4.35 (q, 2H), 3.90 (s, 3H), 3.33 (s, 3H), 2.41 (s, 3H), 1.48 (t, 3H) 5-167 Me OMe SO₂Et 5-168 Me OEt SO₂Me 5-169 Me OEt SO₂Et 5-170 Me OiPr SO₂Me 5-171 Me OiPr SO₂Et 5-172 Me O(CH₂)₂OMe SO₂Me 11.65 (brs, 1H), 7.83 (d, 1H), 7.64 (d, 1H), 4.35 (q, 2H), 4.16 (m, 2H), 3.76 (m, 2H), 3.38 (s, 3H), 3.37 (s, 3H), 2.41 (s, 3H), 1.47 (t, 3H) 5-173 Me O(CH₂)₂OMe SO₂Et 5-174 Me O(CH₂)₃OMe SO₂Me 10.00 (bs, 1H), 7.96 (d, 1H), 7.61 (d, 1H), 4.47 (q, 2H), 4.18 (t, 2H), 3.62 (t, 2H), 3.38 (s, 3H), 3.27 (s, 3H), 2.50 (s, 3H), 2.16 (quin, 2H), 1.64 (t, 3H) 5-175 Me O(CH₂)₃OMe SO₂Et 5-176 Me O(CH₂)₄OMe SO₂Me 5-177 Me O(CH₂)₄OMe SO₂Et 5-178 Me O(CH₂)₂NHSO₂Me SO₂Me 5-179 Me O(CH₂)₂NHSO₂Me SO₂Et 5-180 Me OCH₂(CO)NMe₂ SO₂Me 11.63 (bs, 1H), 7.83 (d, 1H), 7.67 (d, 1H), 4.74 (s, 2H), 4.35 (q, 2H), 3.46 (s, 3H), 2.90 (s, 3H), 2.89 (s, 3H), 2.40 (s, 3H), 1.48 (t, 3H) 5-181 Me OCH₂(CO)NMe₂ SO₂Et 5-182 Me [1,4]dioxan-2- SO₂Me ylmethoxy 5-183 Me [1,4]dioxan-2- SO₂Et ylmethoxy 5-184 Me O(CH₂)₂—O(3,5- SO₂Me dimethoxypyrimidin- 2-yl 5-185 Me Cl SO₂Me 5-186 Me SMe SO₂Me 5-187 Me SOMe SO₂Me 5-188 Me SO₂Me SO₂Me 8.18 (d, 1H), 7.96 (d, 1H), 4.24 (q, 2H), 3.57 (s, 3H), 3.55 (s, 3H), 2.73 (s, 3H), 1.41 (t, 3H) 5-189 Me SO₂Me SO₂Et 5-190 Me SEt SO₂Me 8.13 (d, 1H), 7.76 (d, 1H), 4.47 (q, 2H), 3.47 (s, 3H), 2.92 (q, 2H), 2.79 (s, 3H), 1.64 (t, 3H), 1.29 (t, 3H) 5-191 Me SOEt SO₂Me 8.14 (d, 1H), 7.86 (d, 1H), 4.50 (q, 2H), 3.51 (m, 1H), 3.39 (s, 3H), 3.28 (m, 1H), 2.92 (s, 3H), 1.65 (t, 3H), 1.53 (t, 3H) 5-192 Me SO₂Et SO₂Me 8.28 (d, 1H), 8.09 (d, 1H), 4.33 (q, 2H), 3.72 (q, 2H), 3.59 (s, 3H), 2.73 (s, 3H), 1.46 (t, 3H), 1.37 (t, 3H) 5-193 Me S(CH₂)₂OMe SO₂Me 5-194 Me SO(CH₂)₂OMe SO₂Me 5-195 Me SO₂(CH₂)₂OMe SO2Me 5-196 CH₂SMe OMe SO₂Me 5-197 CH₂OMe OMe SO₂Me 5-198 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 5-199 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 5-200 CH₂O(CH₂)₃OMe OMe SO₂Me 5-201 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 5-202 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 5-203 Et SMe Cl 1.20 (t, 3H), 1.60 (t, 3H), 2.40 (s, 3H), 3.12 (q, 2H), 4.43 (q, 2H), 7.33 (d, 1H), 7.45 (d, 1H) 5-204 Et SO₂Me Cl 1.02 (t, 3H), 1.45 (t, 3H), 3.25 (q, 2H), 3.30 (s, 3H), 4.28 (q, 2H), 7.30 (d, 1H), 7.55 (d, 1H) 5-205 Et SMe CF₃ 1.20 (t, 3H), 1.62 (t, 3H), 3.06 (s, 3H), 3.12 (m, 1H), 3.20 (m, 1H), 4.43 (q, 2H), 7.53 (d, 1H), 7.63 (d, 1H), 10.78 (s, 1H) 5-206 Et SO₂Me CF₃ 1.26 (t, 3H), 1.35 (t, 3H), 3.31 (s, 3H), 3.36 (q, 2H), 4.49 (q, 2H), 7.88 (d, 1H), 7.95 (d, 1H) 5-207 Et F SO₂Me 5-208 Et NH(CH₂)₂OMe SO₂Me 5-209 iPr SO₂Me CF₃ 5-210 cPr SO₂Me CF₃ 5-211 CF₃ O(CH₂)₂OMe F 5-212 CF₃ O(CH₂)₃OMe F 5-213 CF₃ OCH₂CONMe₂ F 5-214 CF₃ [1,4]dioxan-2-F ylmethoxy 5-215 CF₃ O(CH₂)₂OMe Cl 5-216 CF₃ O(CH₂)₃OMe Cl 5-217 CF₃ OCH₂CONMe₂ Cl 5-218 CF₃ [1,4]dioxan-2- Cl ylmethoxy 5-219 CF₃ O(CH₂)₂OMe Br 5-220 CF₃ O(CH₂)₃OMe Br 5-221 CF₃ OCH₂CONMe₂ Br 5-222 CF₃ [1,4]dioxan-2- Br ylmethoxy 5-223 CF₃ O(CH₂)₂OMe I 5-224 CF₃ O(CH₂)₃OMe I 5-225 CF₃ OCH₂CONMe₂ I 5-226 CF₃ [1,4]dioxan-2- I ylmethoxy 5-227 CF₃ F SO₂Me 5-228 CF₃ F SO₂Et 5-229 CF₃ O(CH₂)₂OMe SO₂Me 8.36 (d, 1H), 7.77 (d, 1H), 4.40-4.48 (m, 4H), 3.86 (t, 2H), 3.48 (s, 3H), 3.42 (s, 3H), 3.40 (s, 3H), 1.60 (t, 3H) 5-230 CF₃ O(CH₂)₂OMe SO₂Et 5-231 CF₃ O(CH₂)₃OMe SO₂Me 11.94 (s, 1H), 8.31 (d, 1H), 7.86 (d, 1H), 4.34 (q, 2H), 4.27 (t, 2H), 3.52 (t, 2H), 3.42 (s, 3H), 2.08 (quin, 2H), 1.47 (t, 3H) 5-232 CF₃ O(CH₂)₃OMe SO₂Et 11.93 (s, 1H), 8.29 (d, 1H), 7.87 (d, 1H), 4.35 (q, 2H), 4.26 (t, 2H), 3.55 (t, 2H), 3.53 (t, 2H), 3.27 (s, 3H), 2.06 (quin, 2H), 1.47 (t, 3H), 1.13 (t, 3H) 5-233 CF₃ OCH₂CONMe₂ SO₂Me 11.97 (s, 1H), 8.32 (d, 1H), 7.91 (d, 1H), 4.89 (s, 2H), 4.35 (q, 2H), 3.55 (s, 3H), 2.89 (s, 3H), 2.85 (s, 3H), 1.47 (t, 3H) 5-234 CF₃ OCH₂CONMe₂ SO₂Et 11.95 (s, 1H), 8.31 (d, 1H), 7.91 (d, 1H), 4.87 (s, 2H), 4.35 (q, 2H), 3.75 (q, 2H), 2.88 (s, 3H), 2.84 (s, 3H), 1.47 (t, 3H), 1.09 (t, 3H) 5-235 CF₃ [1,4]dioxan-2- SO₂Me ylmethoxy 5-236 CF₃ [1,4]dioxan-2- SO₂Et ylmethoxy 5-237 F SMe CF₃ 7.79 (t, 1H), 7.58 (d, 1H), 4.11 (q, 2H), 2.43 (s, 3H), 1.33 (t, 3H) 5-238 F SOMe CF₃ 5-239 Cl Me Cl 7.63 (d, 1H), 7.58 (d, 1H), 4.36 (q, 2H), 2.51 (s, 3H), 1.47 (t, 3H) 5-240 Cl OCH₂CHCH₂ Cl 5-241 Cl OCH₂CHF₂ Cl 5-242 Cl O(CH₂)₂OMe Cl 9.51 (bs, 1H), 7.52 (d, 1H), 7.47 (d, 1H), 4.47 (q, 2H), 4.25-4.27 (m, 2H), 3.81-3.84 (m, 2H), 3.47 (s, 3H), 1.63 (t, 3H) 5-243 Cl OCH₂(CO)NMe₂ Cl 5-244 Cl O(CH₂)-5-pyrrolidin- Cl 2-one 5-245 Cl SMe Cl 7.60 (d, 1H), 7.54 (d, 1H), 4.48 (q, 2H), 2.48 (s, 3H), 1.63 (t, 3H) 5-246 Cl SOMe Cl 7.72 (d, 1H), 7.54 (d, 1H), 4.46 (q, 2H), 3.11 (s, 3H), 1.63 (t, 3H) 5-247 Cl SO₂Me Cl 7.71 (d, 1H), 7.66 (d, 1H), 4.52 (q, 2H), 3.43 (s, 3H), 1.63 (t, 3H) 5-248 Cl F SMe 7.69 (dd, 1H), 7.22 (d, 1H), 4.45 (q, 2H), 2.55 (s, 3H), 1.62 (t, 3H) 5-249 Cl Cl SO₂Me 5-250 Cl COOMe SO₂Me 5-251 Cl CONMe₂ SO₂Me 5-252 Cl CONMe(OMe) SO₂Me 5-253 Cl CH₂OMe SO₂Me 1.60 (t, 3H), 3.25 (s, 3H), 3.51 (s, 3H), 4.44 (q, 2H), 5.10 (s, 2H), 7.78 (d, 1H), 8.16 (d, 1H), 11.02 (s, 1H) 5-254 Cl CH₂OMe SO₂Et 5-255 Cl CH₂OEt SO₂Me 1.26 (t, 3H), 1.60 (t, 3H), 3.30 (s, 3H), 3.71 (q, 2H), 4.49 (q, 2H), 5.14 (s, 2H), 7.78 (d, 1H), 8.16 (d, 1H), 10.6 (s, 1H) 5-256 Cl CH₂OEt SO₂Et 5-257 Cl CH₂OCH₂CHF₂ SO₂Me 1.63 (t, 3H), 3.26 (s, 3H), 3.88 (dt, 2H), 4.51 (q, 2H), 5.31 (s, 2H), 7.81 (d, 1H), 8.19 (d, 1H), 10.82 (s, 1H) 5-258 Cl CH₂OCH₂CF₃ SO₂Me 7.94 (d, 1H), 7.65 (d, 1H), 5.25 (s, 2H), 4.33 (t, 2H), 4.01(q, 2H), 3.19 (s, 3H), 1.49 (t, 3H) 5-259 Cl CH₂OCH₂CF₃ SO₂Et 5-260 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 5-261 Cl CH₂Ocpentyl SO₂Me 5-262 Cl CH₂PO(OMe)₂ SO₂Me 5-263 Cl 4,5-dihydro-1,2- SMe oxazol-3-yl 5-264 Cl 4,5-dihydro-1,2- SO₂Me oxazol-3-yl 5-265 Cl 4,5-dihydro-1,2- SO₂Et oxazol-3-yl 5-266 Cl 5-cyanomethyl-4,5- SO₂Me dihydro-1,2-oxazol-3- yl 5-267 Cl 5-cyanomethyl-4,5- SO₂Et dihydro-1,2-oxazol-3- yl 5-268 Cl 5-(methoxymethyl)- SO₂Et 4,5-dihydro-1,2- oxazol-3-yl 5-269 Cl 5-(methoxymethyl)-5- SO₂Et methyl-4,5-dihy-dro- 1,2-oxazol-3-yl 5-270 Cl CH₂O- SO₂Me tetrahydrofuran-3-yl 5-271 Cl CH₂O- SO₂Et tetrahydrofuran-3-yl 5-272 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-2-yl 5-273 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-2-yl 5-274 Cl CH₂OCH₂- SO₂Me tetrahydrofuran-3-yl 5-275 Cl CH₂OCH₂- SO₂Et tetrahydrofuran-3-yl 5-276 Cl OMe SO₂Me 11.92 (bs, 1H), 7.93 (d, 1H), 7.78 (d, 1H), 4.38 (q, 2H), 4.01 (s, 3H), 3.50 (q, 2H), 1.48 (t, 3H), 1.13 (t, 3H) 5-277 Cl OMe SO₂Et 5-278 Cl OEt SO₂Me 10.30 (bs, 1H), 8.04 (d, 1H), 7.62 (d, 1H), 4.51 (q, 2H), 4.36 (q, 2H), 3.31 (s, 3H), 1.64 (t, 3H), 1.55 (t, 3H) 5-279 Cl OEt SO₂Et 11.91 (bs, 1H), 7.94 (d, 1H), 7.77 (d, 1H), 4.38 (q, 2H), 4.24 (q, 2H), 3.52 (q, 2H), 1.48 (t, 3H), 1.45 (t, 3H), 1.12 (t, 3H) 5-280 Cl OiPr SO₂Me 10.25 (bs, 1H), 8.06 (d, 1H), 7.55 (d, 1H), 5.30 (sep, 1H), 4.51 (q, 2H), 3.27 (s, 3H), 1.64 (t, 3H), 1.42 (d, 6H) 5-281 Cl OiPr SO₂Et 11.94 (bs, 1H), 7.95 (d, 1H), 7.70 (d, 1H), 5.15-5.22 (m, 1H), 4.38 (q, 2H), 3.49 (q, 2H), 1.48 (t, 3H), 1.34 (d, 6H), 1.09 (t, 3H) 5-282 Cl O(CH₂)₂OMe SO₂Me 7.97 (d, 1H), 7.77 (d, 1H), 4.38 (q, 2H), 4.32 (m, 2H), 3.80 (m, 2H), 3.40 (s, 3H), 3.39 (s, 3H), 1.48 (t, 3H) 5-283 Cl O(CH₂)₄OMe SO₂Me 5-284 Cl O(CH₂)₄OMe SO₂Et 5-285 Cl O(CH₂)₃OMe SO₂Me 10.65 (bs, 1H), 8.03 (d, 1H), 7.61 (d, 1H), 4.50 (q, 2H), 4.39 (t, 2H), 3.63 (t, 2H), 3.38 (s, 3H), 3.30 (s, 3H), 2.21 (quin, 2H), 1.64 (t, 3H) 5-286 Cl O(CH₂)₃OMe SO₂Et 7.93 (d, 1H), 7.76 (d, 1H), 4.46 (q, 2H), 4.24 (m, 2H), 3.58-3.52 (m, 4H), 3.27(s, 3H), 2.09 (m, 2H), 1.48 (t, 3H), 1.13 (t, 3H) 5-287 Cl O(CH₂)₂OEt SO₂Me 10.65 (bs, 1H), 8.05 (d, 1H), 7.62 (d, 1H), 4.50 (q, 2H), 4.48 (t, 2H), 3.91 (t, 2H), 3.65 (q, 2H), 3.36 (s, 3H), 1.64 (t, 3H), 1.27 (t, 3H) 5-288 Cl O(CH₂)₂OMe SO₂Et 11.91 (bs, 1H), 7.93 (d, 1H), 7.78 (d, 1H), 4.38 (q, 2H), 4.30-4.34 (m, 2H), 3.78 (t, 2H), 3.58 (q, 2H), 3.48 (s, 3H), 1.48 (t, 3H), 1.13 (t, 3H) 5-289 Cl [1,4]dioxan-2- SO₂Me 11.01 (bs, 1H), 7.95 (d, 1H), 7.78 (d, ylmethoxy 1H), 4.38 (q, 2H), 4.20-4.25 (m, 1H), 4.10-4.15 (m, 1H), 4.00-4.05 (m, 1H), 3.89 (dd, 1H), 3.80-3.82 (m, 1H), 3.65-3.70 (m, 2H), 3.45-3.55 (m, 2H), 1.48 (t, 3H) 5-290 Cl [1,4]dioxan-2- SO₂Et 8.02 (d, 1H), 7.62 (d, 1H), 4.51 (q, ylmethoxy 2H), 4.38 (dd, 1H), 4.21 (dd, 1H), 4.10-4.17 (m, 1H), 3.66-3.96 (m, 5H), 3.59 (dd, 1H), 3.49 (q, 2H), 1.63 (t, 3H), 1.28 (t, 3H) 5-291 Cl OCH₂(CO)NMe₂ SO₂Me 11.15 (bs, 1H), 8.04 (d, 1H), 7.67 (d, 1H), 5.02 (s, 2H), 4.49 (q, 2H), 3.45 (s, 3H), 3.04 (s, 3H), 2.96 (s, 3H), 1.63 (t, 3H) 5-292 Cl OCH₂(CO)NMe₂ SO₂Et 11.92 (bs, 1H), 7.95 (d, 1H), 7.81 (d, 1H), 4.89 (s, 2H), 4.38 (q, 2H), 3.70 (q, 2H), 2.89 (s, 3H), 2.88 (s, 3H), 1.48 (t, 3H), 1.11 (t, 3H) 5-293 Cl SMe SO₂Me 5-294 Cl SOMe SO₂Me 5-295 Br OMe Br 10.20 (bs, 1H), 7.68 (d, 1H), 7.33 (d, 1H), 4.50 (q, 2H), 3.95 (s, 3H), 1.64 (t, 3H) 5-296 Br O(CH₂)₂OMe Br 11.72 (brs, 1H), 7.84 (d, 1H), 7.41 (d, 1H), 4.37 (q, 2H), 4.15 (m, 2H), 3.76 (m, 2H), 3.33 (s, 3H), 1.47 (t, 3H) 5-297 Br O(CH₂)₂OMe SO₂Me 5-298 Br O(CH₂)₂OMe SO₂Et 5-299 Br O(CH₂)₃OMe SO₂Me 5-300 Br O(CH₂)₃OMe SO₂Et 5-301 Br O(CH₂)₄OMe SO₂Me 5-302 Br O(CH₂)₄OMe SO₂Et 5-303 Br [1,4]dioxan-2- SO₂Me ylmethoxy 5-304 Br [1,4]dioxan-2- SO₂Et ylmethoxy 5-305 I O(CH₂)₂OMe SO₂Me 5-306 I O(CH₂)₂OMe SO₂Et 5-307 I O(CH₂)₃OMe SO₂Me 5-308 I O(CH₂)₃OMe SO₂Et 5-309 I O(CH₂)₄OMe SO₂Me 5-310 I O(CH₂)₄OMe SO₂Et 5-311 I [1,4]dioxan-2- SO₂Me ylmethoxy 5-312 I [1,4]dioxan-2- SO₂Et ylmethoxy 5-313 OMe SMe CF₃ 5-314 OMe SOMe CF₃ 5-315 OMe SO₂Me CF₃ 5-316 OMe SOEt CF₃ 5-317 OMe SO₂Et CF₃ 5-318 OMe S(CH₂)₂OMe CF₃ 5-319 OMe SO(CH₂)₂OMe CF₃ 5-320 OMe SO₂(CH₂)₂OMe CF₃ 5-321 OMe SMe Cl 5-322 OMe SOMe Cl 5-323 OMe SO₂Me Cl 5-324 OMe SEt Cl 5-325 OMe SOEt Cl 5-326 OMe SO₂Et Cl 5-327 OMe S(CH₂)₂OMe Cl 5-328 OMe SO(CH₂)₂OMe Cl 5-329 OMe SO₂(CH₂)₂OMe Cl 5-330 OCH₂c-Pr SMe CF₃ 5-331 OCH₂c-Pr SOMe CF₃ 5-332 OCH₂c-Pr SO₂Me CF₃ 5-333 OCH₂c-Pr SEt CF₃ 5-334 OCH₂c-Pr SOEt CF₃ 5-335 OCH₂c-Pr SO₂Et CF₃ 5-336 OCH₂c-Pr S(CH₂)₂OMe CF₃ 5-337 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 5-338 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 5-339 OCH₂c-Pr SMe Cl 5-340 OCH₂c-Pr SOMe Cl 5-341 OCH₂c-Pr SO₂Me Cl 5-342 OCH₂c-Pr SEt Cl 5-343 OCH₂c-Pr SOEt Cl 5-344 OCH₂c-Pr SO₂Et Cl 5-345 OCH₂c-Pr S(CH₂)₂OMe Cl 5-346 OCH₂c-Pr SO(CH₂)₂OMe Cl 5-347 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 5-348 OCH₂c-Pr SMe SO₂Me 5-349 OCH₂c-Pr SOMe SO₂Me 5-350 OCH₂c-Pr SO₂Me SO₂Me 5-351 OCH₂c-Pr SEt SO₂Me 5-352 OCH₂c-Pr SOEt SO₂Me 5-353 OCH₂c-Pr SO₂Et SO₂Me 5-354 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 5-355 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 5-356 OCH₂c-Pr SO₂(CH₂)₂OMe SO₂Me 5-357 SO₂Me F CF₃ 5-358 SO₂Me NH₂ CF₃ 5-359 SO₂Me NHEt Cl 5-360 SMe SEt F 5-361 SMe SMe F 5-362 Et H F 11.40 (brs, 1H), 7.72 (dd, 1H), 7.26 (dd, 1H), 7.19 (ddd, 1H), 4.32 (q, 2H), 2.80 (q, 2H), 1.46 (t, 3H), 1.19 (t, 3H) 5-363 CH₂SMe H Br 11.55 (brs, 1H), 7.71 (s, 1H), 7.67 (s, 2H), 4.36 (q, 2H), 3.95 (s, 2H), 1.96 (s, 3H), 1.48 (t, 3H) 5-364 NHSO₂Me H CF₃ 5-365 NHSO₂Et H CF₃ 5-366 NHSO₂CF₃ H CF₃ 5-367 NHSO₂Me H SO₂Me 5-368 NHSO₂Et H SO₂Me 5-369 NHSO₂CF₃ H SO₂Me 5-370 NMeSO₂Me H CF₃ 5-371 NMeSO₂Et H CF₃ 5-372 NMeSO₂CF₃ H CF₃ 5-373 NMeSO₂Me H SO₂Me 5-374 NMeSO₂Et H SO₂Me 5-375 NMeSO₂CF₃ H SO₂Me 5-376 OMe H SO₂Me 11.20 (brs, 1H), 7.92 (d, 1H), 7.65 (d, 1H), 7.64 (dd, 1H), 4.33 (q, 2H), 4.00 (s, 3H), 3.32 (s, 3H), 1.45 (t, 3H) 5-377 OSO₂Me H CF₃ 5-378 OSO₂Et H CF₃ 5-379 OSO₂CF₃ H CF₃ 5-380 OSO₂Me H SO₂Me 5-381 OSO₂Et H SO₂Me 5-382 OSO₂CF₃ H SO₂Me 5-383 Cl H CN 11.90 (brs, 1H), 8.27 (s, 1H), 8.03 (dd, 1H), 7.96 (d, 1H), 4.35 (q, 2H), 1.47 (t, 3H) 5-384 Cl H morpholin-4-yl 7.60 (d, 1H), 7.06 (d, 1H), 7.00 (dd, 1H), 4.30 (q, 2H), 3.73 (m, 4H), 3.28 (m, 4H), 1.45 (t, 3H) 5-385 Cl H 4-methyl-3- 11.75 (brs, 1H), 8.11 (d, 1H), 8.00 trifluoromethyl- (dd, 1H), 7.91 (d, 1H), 4.36 (q, 2H), 1,2,4-triazolin-5- 3.38 (s, 3H), 1.47 (t, 3H) on-1-yl 5-386 Cl H I 11.70 (brs, 1H), 8.05 (d, 1H), 7.90 (dd, 1H), 7.51 (d, 1H), 4.34 (q, 2H), 1.47 (t, 3H) 5-387 SMe H Br 11.50 (brs, 1H), 7.67 (d, 1H), 7.57 (d, 1H), 7.52 (dd, 1H), 4.32 (q, 2H), 2.43 (s, 3H), 1.45 (t, 3H) 5-388 SMe H CF₃ 7.90 (d, 1H), 7.70 (s, 1H), 7.68 (d, 1H), 4.36 (q, 2H), 2.57 (s, 3H), 1.48 (t, 3H) 5-389 SMe H SMe 7.70 (d, 1H), 7.19 (s, 1H), 7.16 (d, 1H), 4.39 (q, 3H), 2.57 (s, 3H), 2.47 (s, 3H), 1.45 (t, 3H) 5-390 SO₂Me H SO₂Me 8.50 (s, 1H), 8.46 (d, 1H), 8.19 (d, 1H), 4.42 (q, 3H), 3.44 (s, 3H), 3.40 (s, 3H), 1.47 (t, 3H) 5-391 Me SOMe Me 9.40 (bs, 1H), 7.68 (d, 1H), 7.45 (d, 1H), 4.46 (q, 2H), 2.82 (s, 3H), 2.38 (s, 3H), 1.63 (t, 3H) 5-392 Me SMe CN 7.76 (d, 1H), 7.72 (d, 1H), 4.50 (q, 2H), 2.76 (s, 3H), 2.53 (s, 3H), 1.63 (t, 3H) (600 MHz) 5-393 Me SOMe CN 7.95 (d, 1H), 7.78 (d, 1H), 4.32 (q, 2H), 3.05 (s, 3H), 2.57 (s, 3H), 1.49 (t, 3H) 5-394 Me SO₂Me CN 7.91 (brs, 2H), 4.48 (q, 2H), 3.31 (s, 3H), 2.89 (s, 3H), 1.64 (t, 3H) 5-395 Me SMe NMe₂ 5-396 Me SOMe NMe₂ 5-397 Me SO₂Me NMe₂ 5-398 Me SMe imidazol-1-yl 5-399 Me SMe 1,2,4-triazol-1-yl 5-400 Me SO₂Me imidazol-1-yl 5-401 Me SOMe 1,2,4-triazol-1-y1 5-402 Me SO₂Me 1,2,4-triazol-1-yl 5-403 Me SMe OMe 5-404 Me SOMe OMe 5-405 Me SO₂Me OMe 5-406 Me SEt OMe 5-407 Me SOEt OMe 5-408 Me SO₂Et OMe 5-409 Me SMe OEt 7.77 (d, 1H), 6.86 (d, 1H), 4.45 (q, 2H), 4.20 (q, 2H), 2.74 (s, 3H), 2.35 (s, 3H), 1.60 (t, 3H), 1.53 (t, 3H) 5-410 Me SOMe OEt 5-411 Me SO₂Me OEt 7.81 (d, 1H), 7.00 (d, 1H), 4.47 (q, 2H), 4.27 (q, 2H), 3.33 (s, 3H), 2.82 (s, 3H), 1.62 (t, 3H), 1.55 (t, 3H) 5-412 Me tetrahydrofuran-2- Cl 11.48 (bs, 1H), 7.50 (d, 1H), 7.43 (d, ylmethoxy 1H), 4.32 (q, 2H), 4.17-4.22 (m, 1H), 3.87-3.89 (m, 2H), 3.81 (q, 1H), 3.72 (q, 1H), 2.38 (s, 3H), 1.99-2.05 (m, 1H), 1.80-1.92 (m, 2H), 1.70-1.77 (m, 1H), 1.46 (t, 3H) 5-413 Me O(CH₂)₃SMe Cl 11.50 (bs, 1H), 7.46 (d, 1H), 7.41 (d, 1H), 4.28 (q, 2H), 3.97 (t, 2H), 2.71 (t, 2H), 2.37 (s, 3H), 2.09 (s, 3H), 2.04 (quin, 2H), 1.43 (t, 3H) 5-414 Me O(CH₂)₂SEt Cl 11.60 (bs, 1H), 7.40 (s, 2H), 4.23 (q, 2H), 4.02 (t, 2H), 2.94 (t, 2H), 2.63 (q, 2H), 2.41 (s, 3H), 1.41 (t, 3H), 1.21 (t, 3H) 5-415 Me O(CH₂)₂SMe Cl 11.50 (bs, 1H), 7.49 (d, 1H), 7.44 (d, 1H), 4.30 (q, 2H), 4.06 (t, 2H), 2.92 (t, 2H), 2.40 (s, 3H), 2.16 (s, 3H), 1.45 (t, 3H) 5-416 Me OEt Cl 11.44 (bs, 1H), 7.50 (d, 1H), 7.42 (d, 1H), 4.32 (q, 2H), 3.97 (q, 2H), 2.37 (s, 3H), 1.46 (t, 3H), 1.39 (t, 3H) 5-417 Me OMe Cl 11.50 (bs, 1H), 7.50 (d, 1H), 7.43 (d, 1H), 4.31 (q, 2H), 3.78 (s, 3H), 2.37 (s, 3H), 1.46 (t, 3H) 5-418 Me O(CH₂)₂N(Me)SO₂Me Cl 11.50 (bs, 1H), 7.50 (d, 1H), 7.45 (d, 1H), 4.32 (q, 2H), 4.04 (t, 2H), 3.54 (t, 2H), 2.96 (s, 3H), 2.94 (s, 3H), 2.39 (s, 3H), 1.46 (t, 3H) 5-419 Me tetrahydrofuran-2- Br 11.45 (bs, 1H), 7.64 (d, 1H), 7.35 (d, ylmethoxy 1H), 4.32 (q, 2H), 4.18-4.25 (m, 1H), 3.87 (d, 2H), 3.79-3.85 (m, 1H), 3.69- 3.75 (m, 1H), 2.40 (s, 3H), 1.98-2.05 (m, 1H), 1.73-1.90 (m, 3H), 1.46 (t, 3H) 5-420 Me OEt Br 11.45 (bs, 1H), 7.64 (d, 1H), 7.34 (d, 1H), 4.32 (q, 2H), 3.95 (q, 2H), 2.33 (s, 3H), 1.46 (t, 3H), 1.40 (t, 3H) 5-421 Me O(CH₂)₂OMe Br 9.52 (bs, 1H), 7.56 (d, 1H), 7.37 (d, 1H), 4.45 (q, 2H), 4.10-4.12 (m, 2H), 3.79-3.81 (m, 2H), 3.47 (s, 3H), 2.53 (s, 3H), 1.62 (t, 3H) 5-422 Me O(CH₂)₃OMe Br 9.50 (bs, 1H), 7.56 (d, 1H), 7.37 (d, 1H), 4.45 (q, 2H), 4.01 (t, 2H), 3.65 (t, 2H), 3.38 (s, 3H), 2.50 (s, 3H), 2.13 (quin, 2H), 1.62 (t, 3H) 5-423 Me O(CH₂)₃SMe Br 11.60 (bs, 1H), 7.58 (d, 1H), 7.33 (d, 1H), 4.26 (q, 2H), 3.94 (t, 2H), 2.72 (t, 2H), 2.39 (s, 3H), 2.09 (s, 3H), 2.05 (quin, 2H), 1.42 (t, 3H) 5-424 Me O(CH₂)₂SEt Br 11.60 (bs, 1H), 7.52 (d, 1H), 7.31 (d, 1H), 4.20 (q, 2H), 4.00 (t, 2H), 2.95 (t, 2H), 2.63 (q, 2H), 2.42 (s, 3H), 1.39 (t, 3H), 1.22 (t, 3H) 5-425 Me O(CH₂)₂SMe Br 11.49 (bs, 1H), 7.65 (d, 1H), 7.37 (d, 1H), 4.31 (q, 2H), 4.04 (t, 2H), 2.93 (t, 2H), 2.42 (s, 3H), 2.17 (s, 3H), 1.45 (t, 3H) 5-426 Me 1,4-dioxan-2- Br 11.50 (bs, 1H), 7.65 (d, 1H), 7.37 (d, ylmethoxy 1H), 4.31 (q, 2H), 3.87-3.91 (m, 4H), 3.79-3.81 (m, 1H), 3.66-3.69 (m, 2H), 3.48-3.52 (m, 2H), 2.38 (s, 3H), 1.46 (t, 3H) 5-427 Me OMe Br 11.49 (bs, 1H), 7.65 (d, 1H), 7.37 (d, 1H), 4.32 (q, 2H), 3.77 (s, 3H), 3.28 (s, 3H), 1.46 (t, 3H) 5-428 Me Me SMe 11.35 (brs, 1H), 7.46 (d, 1H), 7.19 (d, 1H), 4.32 (q, 2H), 2.43 (s, 3H), 2.34 (s, 3H), 2.26 (s, 3H), 1.46 (t, 3H) 5-429 Me F SMe 7.68 (d, 1H), 7.31 (t, 1H), 4.31 (q, 2H), 2.54 (s, 3H), 2.34 (d, 3H), 1.46 (t, 3H) 5-430 Me NHEt SO₂Me 1.30 (t, 3H), 1.63 (t, 3H), 2.46 (s, 3H), 3.10 (s, 3H), 3.28 (q, 2H), 4.47 (q, 2H), 5.56 (s, br, 1H), 7.26 (d, 1H), 7.79 (d, 1H), 10.62 (s, 1H) 5-431 Me NHnPr SO₂Me 1.03 (t, 3H), 1.63 (t, 3H), 1.71 (m, 2H), 2.46 (s, 3H), 3.09 (s, 3H), 3.19 (t, 2H), 4.47 (q, 2H), 5.66 (s, br, 1H), 7.24 (d, 1H), 7.79 (d, 1H), 10.58 (s, 1H) 5-432 Me N(CH₃)CH₂cPr SO₂Me 0.12 (m, 1H), 0.22 (m, 1H), 0.47 (m, 1H), 0.63 (m, 1H), 1.09 (m, 1H), 1.63 (t, 3H), 2.44 (s, 3H), 2.65 (m, 1H), 2.95 (s, 3H), 3.19 (m, 1H), 3.34 (s, 3H), 4.46 (q, 2H), 7.59 (d, 1H), 7.92 (d, 1H) 5-433 Me NH(CH₂)₂OEt SO₂Me 1.22 (t, 3H), 1.63 (t, 3H), 2.45 (s, 3H), 3.20 (s, 3H), 3.41 (m, 2H), 3.56 (q, 2H), 3.65 (m, 2H), 4.56 (q, 2H), 5.85 (s, 1H), 7.25 (d, 1H), 7.77 (d, 1H), 10.46 (s, 1H) 5-434 Me NHCH₂CH(OMe)₂ SO₂Me 1.63 (t, 3H), 2.46 (s, 3H), 3.19 (s, 3H), 3.38 (m, 2H), 3.43 (s, 3H), 4.46 (q, 2H), 4.54 (t, 1H), 5.80 (t, br, 1H), 7.25 (d, 1H), 7.78 (d, 1H), 10.57 (s, br, 1H) 5-435 Me NHCH₂CH₂(1,3- SO₂Me 1.38 (dd, 1H), 1.63 (t, 3H), 1.98 dioxan-2-yl) (m, 2H), 2.12 (m, 1H), 2.45 (s, 3H), 3.15 (s, 3H), 3.32 (s, br, 2H), 3.80 (m, 2H), 4.13 (m, 2H), 4.46 (q, 2H), 4.78 (t, 1H), 5.72 (s, br, 1H), 7.28 (d, 1H), 7.78 (d, 1H), 10.47 (s, 1H) 5-436 Me NHCH₂(4-methyl- SO₂Me 1.29 and 1.37 (d and d, 3H), 1.61 1,3-dioxolan-2-yl) (t, 3H), 2.46 (s, 3H), 3.18 (s, 3H), 3.48 (m, 1H), 3.52 (m, 2H), 4.03 (t, 1H), 4.25 and 4.38 (m and m, 1H), 4.47 (q, 2H), 5.14 and 5.23 (t and t, 1H), 5.97 (t, br, 1H), 7.24 (d, 1H), 7.75(dd, 1H), 10.70 (s, 1H) 5-437 Me NHCO₂(CH₂)₂OMe SO₂Me 11.74 (brs, 1H), 9.30 (brs, 1H), 7.95 (d, 1H), 7.82 (d, 1H), 4.35 (q, 2H), 4.21 (m, 2H), 3.57 (m, 2H), 3.31 (s, 1H), 3.25 (s, 3H), 2.29 (s, 3H), 1.47 (t, 3H) 5-438 Me NHCONMeCH₂iPr SO₂Me 11.65 (brs, 1H), 7.77 (d, 1H), 7.25 (d, 1H), 5.60. 5.57 (2s, 1H), 4.34 (q, 2H), 3.69 (m, 1H), 3.29 (s, 1H), 3.17-3.0 (m, 2H), 2.32, 2.25 (2s, 3H), 1.47 (t, 3H), 1.15, 0.88 (2d, 6H) 5-439 Me NHCH₂CONHEt SO₂Me 11.70 (brs, 1H), 8.13 (t, 1H), 7.72 (d, 1H), 7.26 (d, 1H), 6.18 (t, 1H), 4.34 (q, 2H), 3.88 (d, 2H), 3.33 (s, 1H), 3.14 (m, 2H), 2.32 (s, 3H), 1.47 (t, 3H), 1.04 (t, 3H) 5-440 Me NHCH₂- SO₂Me 11.70 (brs, 1H), 7.73 (d, 1H), 7.28 tetrahydrofuran-2-yl (d, 1H), 5.73 (t, 1H), 4.43 (q, 2H), 4.03 (m, 1H), 3.82 (m, 1H), 3.69 (m, 1H), 3.36-3.27 (m, 1H), 3.31 (s, 1H), 3.13 (m, 1H), 2.34 (s, 3H), 2.02-1.55 (m, 4H), 1.47 (t, 3H) 5-441 Me 3-methyl- SO₂Me 11.74 (brs, 1H), 7.96 (d, 1H), 7.83 tetrahydropyrimid-2- (d, 1H), 4.36 (q, 2H), 3.53-3.33 on-1-yl (m, 4H), 3.19 (s, 3H), 2.90 (s, 3H), 2.28 (s, 3H), 2.18-2.01 (m, 2H), 1.47 (t, 3H) 5-442 Me pyrrolidin-2-on-1-yl SO₂Me 11.80 (brs, 1H), 8.01 (d, 1H), 7.90 (d, 1H), 4.35 (q, 2H), 3.75-3.61 (m, 2H), 3.20 (s, 3H), 2.59-2.39 (m, 2H), 2.28 (s, 3H), 2.23-2.17 (m, 2H), 1.47 (t, 3H) 5-443 Me pyrazol-1-yl SO₂Me 5-444 Me 4-methoxypyrazol-1- SO₂Me 11.80 (brs, 1H), 8.10 (d, 1H), 8.05 yl (d, 1H), 7.76 (s, 1H), 7.67 (s, 1H), 4.36 (q, 2H), 3.75 (s, 3H), 3.12 (s, 3H), 1.97 (s, 3H), 1.47 (t, 3H) 5-445 Me 4-Me-pyrazol-1-yl SO₂Me 5-446 Me 3,5-d imethyl-pyrazol- SO₂Me 8.09 (d, 1H), 8.05 (d, 1H), 6.13 (s, 1H), 1-yl 4.35 (q, 2H), 3.17 (s, 3H), 2.22 (s, 3H), 1.99 (s, 3H), 1.87 (s, 3H), 1.47 (t, 3H) 5-447 Me 4-CN-pyrazol-1-yl SO₂Me 5-448 Me 4-Cl-pyrazol-1-yl SO₂Me 5-449 Me 1,2,3-triazol-1-yl SO₂Me 5-450 Me 1,2,4-triazol-1-yl SO₂Me 5-451 Me 5-iPr-1,2,4-triazol-1- SO₂Me yl 5-452 Me 5-EtS-1,2,4-triazol- SO₂Me 1-yl 5-453 Me O(CH₂)₃SMe SO₂Me 11.62 (bs, 1H), 7.83 (d, 1H), 7.63 (d, 1H), 4.35 (q, 2H), 4.10 (t, 2H), 3.34 (s, 3H), 2.71 (t, 2H), 2.41 (s, 3H), 2.12 (quin, 2H), 2.10 (s, 3H), 1.48 (t, 3H) 5-454 Me O(CH₂)₂SEt SO₂Me 11.62 (bs, 1H), 7.83 (d, 1H), 7.64 (d, 1H), 4.35 (q, 2H), 4.15 (t, 2H), 3.38 (s, 3H), 3.02 (t, 2H), 2.63 (q, 2H), 2.43 (s, 3H), 1.48 (t, 3H), 1.23 (t, 3H) 5-455 Me O(CH₂)₂SMe SO₂Me 11.62 (bs, 1H), 7.83 (d, 1H), 7.64 (d, 1H), 4.35 (q, 2H), 4.17 (t, 2H), 3.39 (s, 3H), 2.99 (t, 2H), 2.44 (s, 3H), 2.17 (s, 3H), 1.48 (t, 3H) 5-456 Me tetrahydrofuran-2- SO₂Me 10.44 (bs, 1H), 7.97 (d, 1H), 7.65 (d, ylmethoxy 1H), 4.47 (q, 2H), 4.40-4.43 (m, 1H), 4.07-4.11 (m, 2H), 3.97 (dd, 1H), 3.88 (dd, 1H), 3.32 (s, 3H), 2.55 (s, 3H), 2.00-2.11 (m, 1H), 1.95-1.99 (m, 2H), 1.67-1.73 (m, 1H), 1.63 (t, 3H) 5-457 Me SCH₂CF₃ SO₂Me 5-458 Me SOCH₂CF₃ SO₂Me 5-459 Me SO₂CH₂CF₃ SO₂Me 5-460 Me SMe SO₂Et 5-461 Me SOMe SO₂Et 5-462 Me SEt SO₂Et 5-463 Me SOEt SO₂Et 5-464 Me SO₂Et SO₂Et 5-465 Me S(CH₂)₂OMe SO₂Et 5-466 Me SO(CH₂)₂OMe SO₂Et 5-467 Me SO₂(CH₂)₂OMe SO₂Et 5-468 Me S(4-F—Ph) SO₂Me 5-469 Me SO(4-F—Ph) SO₂Me 5-470 Me SO₂(4-F—Ph) SO₂Me 5-471 Et SOMe CF₃ 1.25 (t, 3H), 1.65 (t, 3H), 3.04 (s, 3H), 3.42 (m, 1H), 3.62 (m, 1H), 4.48 (q, 2H), 7.72 (d, 1H), 7.81 (d, 1H) 5-472 Et SEt CF₃ 5-473 Et SOEt CF₃ 5-474 Et SO₂Et CF₃ 5-475 Et S(CH₂)₂OMe CF₃ 5-476 Et SO(CH₂)₂OMe CF₃ 5-477 Et SO₂(CH₂)₂OMe CF₃ 5-478 Et SEt Cl 7.58 (d, 1H), 7.48 (d, 1H), 4.47 (q, 2H), 3.20 (q, 2H), 2.91 (q, 2H), 1.62 (t, 3H), 1.25-1.19 (m, 6H) 5-479 Et SOEt Cl 7.64 (d, 1H), 7.38 (d, 1H), 4.43 (q, 2H), 3.57 (m, 1H), 3.20-2.95 (m, 3H), 1.62 (t, 3H), 1.39 (t, 3H), 1.18 (t, 3H) 5-480 Et SO₂Et Cl 7.62 (d, 1H), 7.52 (d, 1H), 4.45 (q, 2H), 3.51 (q, 2H), 3.30 (q, 2H), 1.60 (t, 3H), 1.37 (t, 3H), 1.27 (t, 3H) 5-481 Et S(CH₂)₂OMe Cl 5-482 Et SO(CH₂)₂OMe Cl 5-483 Et SO₂(CH₂)₂OMe Cl 5-484 Et SOMe Cl 1.2 (t, 3H), 1.42 (t, 3H), 3.08 (s, 3H), 3.18 (m, 1H), 3.23 (m, 1H), 4.28 (q, 2H), 7.52 (d, 1H), 7.70 (d, 1H) 5-485 Et SMe Br 1.23 (t, 3H), 1.62 (t, 3H), 2.42 (s, 3H), 3.20 (q, 2H), 4.46 (q, 3H), 7.52 (d, 1H), 7.69 (d, 1H), 10.68 (s, 1H) 5-486 Et SOMe Br 1.25 (t, 3H), 3.10 (s, 3H), 3.19 (m, 1H), 3.35 (m, 1H), 4.13 (s, 3H), 7.55 (d, 1H), 7.65 (d, 1H), 5-487 Et SO₂Me Br 1.06 (t, 3H), 1.48 (t, 3H), 3.26 (q, 2H), 3.32 (s, 3H), 4.30 (q, 2H), 7.45 (d, 1H), 7.59 (d, 1H), 8.55 (s, 1H) 5-488 Et SEt SO₂Me 5-489 Et SOEt SO₂Me 5-490 Et SO₂Et SO₂Me 5-491 Et S(CH₂)₂OMe SO₂Me 5-492 Et SO(CH₂)₂OMe SO₂Me 5-493 Et SO₂(CH₂)₂OMe SO₂Me 5-494 Et SMe SO₂Et 5-495 Et SOMe SO₂Et 5-496 Et SO₂Me SO₂Et 5-497 Et SEt SO₂Et 5-498 Et SOEt SO₂Et 5-499 Et SO₂Et SO₂Et 5-500 Et S(CH₂)₂OMe SO₂Et 5-501 Et SO(CH₂)₂OMe SO₂Et 5-502 Et SO₂(CH₂)₂OMe SO₂Et 5-503 Et SMe SO₂Me 5-504 Et SOMe SO₂Me 5-505 Et SO₂Me SO₂Me 5-506 nPr SMe CF₃ 0.92 (t, 3H), 1.35 (t, 3H), 1.62 (m, 2H), 2.25 (s, 3H), 3.10 (m, 2H), 4.15 (q, 2H), 7.62 (m, 2H) 5-507 nPr SOMe CF₃ 0.96 (t, 3H), 1.52 (m, 1H), 1.64 (t, 3H), 1.71 (m, 1H), 3.04 (s, 3H), 3.28 (m, 1H), 3.58 (m, 1H), 4.47 (q, 2H), 7.73 (d, 1H), 7.81 (d, 1H), 10.90 (br, s, 1H) 5-508 nPr SO₂Me CF₃ 0.98 (t, 3H), 1.64 (t, 3H), 1.67 (m, 2H), 3.25 (m, 2H), 3.30 (s, 3H), 4.47 (q, 2H), 7.91 (s, 2H), 10.6 (br, s, 1H) 5-509 nPr SMe Cl 0.96 (t, 3H), 1.60 (m, 2H), 1.62 (t, 3H), 2.41 (s, 3H), 3.13 (m, 2H), 4.46 (q, 2H), 7.49 (d, 1H), 7.61 (d, 1H), 10.75 (s, 1H) 5-510 nPr SOMe Cl 0.97 (t, 3H), 1.39 (m, 1H), 1.61 (t, 3H), 1.62 (m, 1H), 2.88 (m, 1H), 3.05 (m, 1H), 3.08 (s, 3H), 4.42 (q, 3H), 7.40 (d, 1H), 7.65 (d, 1H), 11.0 (br, s, 1H) 5-511 nPr SO₂Me Cl 0.92 (t, 3H), 1.62 (t, 3H), 1.65 (m, 2H), 3.22 (m, 2H), 3.37 (s, 3H), 4.46 (q, 2H), 7.52 (d, 1H), 7.63 (d, 1H), 10.65 (s, 1H) 5-512 nPr SMe Br 0.96 (t, 3H), 1.60 (t, 3H), 1.61 (m, 2H), 2.41 (s, 3H), 3.15 (m, 2H), 4.46 (q, 3H), 7.51 (d, 1H), 7.69 (d, 1H) 5-513 nPr SOMe Br 0.97 (t, 3H), 1.47 (m, 1H), 1.58 (m, 1H), 1.62 (t, 3H), 2.99 (m, 1H), 3.06 (s, 3H), 3.13 (m, 1H), 4.43 (q, 2H), 7.53 (d, 1H), 7.61 (d, 1H), 10.78 (s, 1H) 5-514 nPr SO₂Me Br 0.92 (t, 3H), 1.62 (t, 3H), 1.65 (m, 2H), 3.23 (m, 2H), 3.38 (s, 3H), 4.45 (q, 2H), 7.52 (d, 1H), 7.75 (d, 1H), 10.60 (s, 1H) 5-515 nPr SMe SO₂Me 5-516 nPr SOMe SO₂Me 5-517 nPr SO₂Me SO₂Me 5-518 iPr SMe CF₃ 5-519 iPr SOMe CF₃ 5-520 iPr SMe Cl 1.43 (d, 6H), 1.62 (t, 3H), 2.41 (s, 3H), 3.88 (br, s, 1H), 4.48 (q, 2H), 7.43 (br, m, 2H), 10.28 (s, 1H) 5-521 iPr SOMe Cl 1.38 (m, 6H), 1.60 (t, 3H), 3.09 (s, 3H), 3.88 (br, s, 1H), 4.42 (q, 2H), 7.38 (d, 1H), 7.51 (d, 1H) 5-522 iPr SO₂Me Cl 1.21 (d, 6H), 1.45 (t, 3H), 3.30 (s, 3H), 4.02 (m, 1H), 4.28 (q, 2H), 7.31 (d, 1H), 7.45 (d, 1H) 5-523 iPr SMe Br 5-524 iPr SOMe Br 5-525 iPr SO₂Me Br 5-526 iPr SMe SO₂Me 5-527 iPr SOMe SO₂Me 5-528 iPr SO₂Me SO₂Me 5-529 cPr SMe CF₃ 5-530 cPr SOMe CF₃ 5-531 cPr SO₂Me CF₃ 0.75 (d, 2H), 1.05 (d, 2H), 1.48 (t, 3H), 2.68 (m, 1H), 3.58 (s, 3H), 4.38 (q, 2H), 8.0 (m, 2H), 11.7 (br, s, 1H) 5-532 cPr SMe Cl 0.61 (m, 1H), 1.12 (m, 1H), 1.64 (t, 3H), 2.41 (m, 1H), 2.50 (s, 3H), 4.49 (q, 2H), 7.44 (s, 2H), 11.13 (s, 1H) 5-533 cPr SOMe Cl 5-534 cPr SO₂Me Cl 5-535 cPr SMe Br 5-536 cPr SOMe Br 5-537 cPr SO₂Me Br 5-538 cPr SMe SO₂Me 5-539 cPr SOMe SO₂Me 5-540 cPr SO₂Me SO₂Me 5-541 CH₂OMe F CF₃ 5-542 CH₂OMe SMe CF₃ 5-543 CH₂OMe SOMe CF₃ 5-544 CH₂OMe SO₂Me CF₃ 5-545 CH₂OMe SEt CF₃ 5-546 CH₂OMe SOEt CF₃ 5-547 CH₂OMe SO₂Et CF₃ 5-548 CH₂OMe S(CH₂)₂OMe CF₃ 5-549 CH₂OMe SO(CH₂)₂OMe CF₃ 5-550 CH₂OMe SO₂(CH₂)₂OMe CF₃ 5-551 CH₂OMe SMe Cl 5-552 CH₂OMe SOMe Cl 5-553 CH₂OMe SO₂Me Cl 5-554 CH₂OMe SEt Cl 5-555 CH₂OMe SOEt Cl 5-556 CH₂OMe SO₂Et Cl 5-557 CH₂OMe S(CH₂)₂OMe Cl 5-558 CH₂OMe SO(CH₂)₂OMe Cl 5-559 CH₂OMe SO₂(CH₂)₂OMe Cl 5-560 CH₂OMe Cl SO₂Me 8.33 (d, 1H), 7.90 (d, 1H), 4.92 (s, 2H), 4.45 (q, 2H), 3.65 (s, 3H), 3.34 (s, 3H), 1.64 (t, 3H) 5-561 CH₂OMe SMe SO₂Me 5-562 CH₂OMe SOMe SO₂Me 5-563 CH₂OMe SO₂Me SO₂Me 5-564 CH₂OMe SEt SO₂Me 5-565 CH₂OMe SOEt SO₂Me 5-566 CH₂OMe SO₂Et SO₂Me 5-567 CH₂OMe S(CH₂)₂OMe SO₂Me 5-568 CH₂OMe SO(CH₂)₂OMe SO₂Me 5-569 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 5-570 CH₂OMe SMe SO₂Et 5-571 CH₂OMe SOMe SO₂Et 5-572 CH₂OMe SO₂Me SO₂Et 5-573 CH₂OMe SEt SO₂Et 5-574 CH₂OMe SOEt SO₂Et 5-575 CH₂OMe SO₂Et SO₂Et 5-576 CH₂OMe S(CH₂)₂OMe SO₂Et 5-577 CH₂OMe SO(CH₂)₂OMe SO₂Et 5-578 CH₂OMe SO₂(CH₂)₂OMe SO₂Et 5-579 CF₃ OEt SO₂Me 12.04 (s, 1H), 8.30 (d, 1H), 7.87 (d, 1H), 4.26 (q, 2H), 3.99 (s, 3H), 3.42 (s, 3H), 1.45 (t, 3H) 5-580 CF₃ O(CH₂)₂SMe SO₂Me 11.92 (s, 1H), 8.31 (d, 1H), 7.87 (d, 1H), 4.32-4.37 (m, 4H), 3.47 (s, 3H), 2.99 (t, 2H), 2.15 (s, 3H), 1.45 (t, 3H) 5-581 CF₃ O(CH₂)₂SMe SO₂Et 11.91 (s, 1H), 8.30 (d, 1H), 7.88 (d, 1H), 4.32-4.37 (m, 4H), 3.62 (q, 2H), 2.96 (t, 2H), 2.14 (s, 3H), 1.47 (t, 3H), 1.14 (t, 3H) 5-582 CF₃ O(CH₂)₃SEt SO₂Me 11.92 (s, 1H), 8.31 (d, 1H), 7.86 (d, 1H), 4.35 (q, 2H), 4.28 (t, 2H), 3.41 (s, 3H), 2.69 (t, 2H), 2.55 (q, 2H), 2.11 (quin, 2H), 1.47 (t, 3H), 1.20 (t, 3H) 5-583 CF₃ O(CH₂)₃SEt SO₂Et 11.91 (bs, 1H), 8.29 (d, 1H), 7.87 (d, 1H), 4.35 (q, 2H), 4.27 (t, 2H), 3.53 (q, 2H), 2.68 (t, 2H), 2.52 (t, 2H), 2.09 (quin, 2H), 1.47 (t, 3H), 1.20 (t, 3H), 1.13 (t, 3H) 5-584 CF₃ OCH₂(CO)N(Me)Et SO₂Me 11.96 (s, 1H), 8.32 (d, 1H), 7.90 (d, 1H), 4.91 (s, 1H), 4.85 (s, 1H), 4.30- 4.37 (m, 2H), 3.55 (s, 3H), 2.87-3.18 (m, 2H), 2.87 (s, 1.5H), 2.82 (s, 1.5H), 1.47 (t, 3H), 1.03-1.07 (m, 3H) 5-585 CF₃ OCH₂(CO)N(Me)Et SO₂Et 11.95 (s, 1H), 8.31 (d, 1H), 7.91 (d, 1H), 4.89 (s, 1H), 4.84 (s, 1H), 4.35 (q, 2H), 3.75 (q, 2H), 3.17 (q, 2H), 2.86 (s, 1.5H), 2.82 (s, 1.5H), 1.47 (t, 3H), 1.03-1.16 (m, 6H) 5-586 CF₃ 2-(1H-pyrazol-1- SO₂Me 11.93 (s, 1H), 8.29 (d, 1H), 7.90 (d, yl)ethoxy 1H), 7.84 (d, 1H), 7.51 (d, 1H), 6.29 (t, 1H), 4.60-4.62 (m, 2H), 4.53-4.55 (m, 2H), 4.33 (q, 2H), 3.29 (s, 3H), 1.46 (t, 3H) 5-587 CF₃ 2-(1H-pyrazol-1- SO₂Et 11.92 (s, 1H), 8.28 (d, 1H), 7.88 (d, yl)ethoxy 1H), 7.82 (d, 1H), 7.51 (d, 1H), 6.29 (t, 1H), 4.58-4.65 (m, 2H), 4.50-4.54 (m, 2H), 4.34 (q, 2H), 3.28-3.36 (m, 2H), 1.46 (t, 3H), 1.05 (t, 3H) 5-588 CF₃ tetrahydrofuran-2- SO₂Me 11.94 (s, 1H), 8.32 (d, 1H), 7.87 (d, ylmethoxy 1H), 4.34 (q, 2H), 4.27-4.31 (m, 1H), 4.23 (t, 1H), 4.13 (dd, 1H), 3.72-3.84 (m, 2H), 3.49 (s, 3H), 1.98-2.05 (m, 1H), 1.83-1.91 (m, 2H), 1.69-1.74 (m, 1H), 1.47 (t, 3H) 5-589 CF₃ tetrahydrofuran-2- SO₂Et 11.93 (s, 1H), 8.31 (d, 1H), 7.88 (d, ylmethoxy 1H), 4.32 (q, 2H), 4.25-4.30 (m, 1H), 4.22 (t, 1H), 4.10 (dd, 1H), 3.70-3.83 (m, 2H), 3.64 (q, 2H), 1-95-2.05 (m, 1H), 1.80-1.90 (m, 2H), 1.65-1.73 (m, 1H), 1.47 (t, 3H), 1.13 (t, 3H) 5-590 CF₃ 2-(2-thienyl)ethoxy SO₂Me 11.96 (bs, 1H), 8.31 (d, 1H), 7.88 (d, 1H), 7.41 (d, 1H), 7.00-7.02 (m, 2H), 4.41 (t, 2H), 4.34 (q, 2H), 3.40 (t, 2H), 3.29 (s, 3H), 1.46 (t, 3H) 5-591 CF₃ 2-(2-thienyl)ethoxy SO₂Et 11.95 (bs, 1H), 8.30 (d, 1H), 7.89 8d, 1H), 7.41 (d, 1H), 7.00-7.02 (m, 2H), 4.40 (t, 2H), 4.35 (q, 2H), 3.40 (q, 2H), 1.47 (t, 3H), 1.08 (t, 3H) 5-592 CF₃ 2-(1H-1,2,3-triazol- SO₂Et 11.05 (bs, 1H), 8.29 (d, 1H), 8.25 (s, 1-yl)ethoxy 1H), 7.91 (d, 1H), 7.80 (s, 1H), 4.89 (t, 2H), 4.55 (t, 2H), 4.34 (q, 2H), 1.46 (t, 3H), 1.06 (t, 3H) 5-593 CF₃ 1,3-dioxolan-4- SO₂Me 12.00 (bs, 1H), 8.30 (bs, 1H), 7.97 ylmethoxy (bs, 1H), 4.85 (d, 1H), 4.76 (d, 1H), 4.50-4.55 (m, 1H), 4.33- 4.37 (m, 4H), 4.10-4.12 (m, 2H), 3.97-4.00 (m, 2H), 3.50 (s, 3H), 1.47 (t, 3H) 5-594 CF₃ 1,3-d ioxolan-4- SO₂Et 11.98 (bs, 1H), 8.34 (d, 1H), 7.88 (d, ylmethoxy 1H), 4.85 (d, 1H), 4.75 (d, 1H), 4.50- 4.54 (m, 1H), 4.33-4.38 (m, 3H), 4.10 (dd, 2H), 3.96-4.00 (m, 2H), 1.47 (t, 3H), 1.11 (t, 3H) 5-595 CF₃ tetrahydro-2H- SO₂Me 11.96 (bs, 1H), 8.31 (d, 1H), 7.87 (d, pyran-2-ylmethoxy 1H), 4.35 (q, 2H), 4.26 (t, 1H), 4.08 (dd, 1H), 3.94 (dd, 1H), 3.75-3.79 (m, 1H), 3.49 (s, 3H), 3.41-3.46 (m, 1H), 1.80-1.85 (m, 1H), 1.60-1.64 (m, 1H), 1.45-1.59 (m, 3H), 1.48 (t, 3H), 1.31- 1.35 (m, 1H) 5-596 CF₃ tetrahydro-2H- SO₂Et 11.95 (bs, 1H), 8.30 (d, 1H), 7.88 (d, pyran-2-ylmethoxy 1H), 4.35 (q, 2H), 4.24 (dd, 1H), 4.06 (dd, 1H), 3.93 (dd, 1H), 3.73-3.79 (m, 1H), 3.61-3.66 (m, 2H), 3.40-3.45 (m, 1H), 1.80-1.85 (m, 1H), 1.59-1.63 (m, 1H), 1.48-1.56 (m, 3H), 1.31 (t, 3H), 1.29-1.33 (m, 1H), 1.12 (t, 3H) 5-597 CF₃ SMe SO₂Me 11.93 (s, 1H), 8.49 (d, 1H), 8.14 (d, 1H), 4.35 (q, 2H), 3.63 (s, 3H), 2.54 (s, 3H), 1.48 (t, 3H) 5-598 CF₃ SMe SO₂Et 11.97 (s, 1H), 8.48 (d, 1H), 8.15 (d, 1H), 4.35 (q, 2H), 3.81 (q, 2H), 2.52 (s, 3H), 1.48 (t, 3H), 1.16 (t, 3H) 5-599 NO₂ SO₂Me Me 12.08 (bs, 1H), 8.22 (d, 1H), 7.91 (d, 1H), 4.29 (q, 2H), 3.47 (s, 3H), 2.79 (s, 3H), 1.45 (t, 3H) 5-600 NO₂ SO₂Et Me 11.40 (bs, 1H), 8.08 (d, 1H), 7.62 (d, 1H), 4.37 (q, 2H), 3.45 (q, 2H), 2.84 (s, 3H), 1.59 (t, 3H), 1.48 (t, 3H) 5-601 NO₂ SOMe Me 12.02 (bs, 1H), 8.06 (d, 1H), 7.77 (d, 1H), 4.28 (m, 1H), 3.42-3.53 (m, 1H), 3.18-3.28 (m, 1H), 3.61 (s, 3H), 1.44 (t, 3H), 1.32 (t, 3H) 5-602 NO₂ SOMe Me 12.02 (bs, 1H), 8.04 (d, 1H), 7.76 (d, 1H), 4.27 (q, 2H), 3.14 (s, 3H), 2.61 (s, 3H), 1.44 (t, 3H) 5-603 NO₂ SEt Me 7.95 (d, 1H), 7.34 (d, 1H), 4.30 (q, 2H), 2.76 (q, 2H), 2.58 (s, 3H), 1.49 (t, 2H), 1.18 (t, 3H) 5-604 NO₂ SMe Me 7.94 (bs, 1H), 7.33 (d, 1H), 4.31 (q, 2H), 2.58 (s, 3H), 2.30 (s, 3H), 1.50 (t, 3H) 5-605 F SMe Br 11.58 (bs, 1H), 7.74 (d, 1H), 7.67 (dd, 1H), 4.32 (q, 2H), 2.48 (s, 3H), 1.46 (t, 3H) 5-606 F SCH₂Ph CF₃ 5-607 F SMe F 5-608 F SOMe F 5-609 F SO₂Me F 5-610 Cl SO₂Me H 5-611 Cl SCF₂CF₂H H 5-612 Cl SOCF₂CF₂H H 5-613 Cl SO₂CF₂CF₂H H 5-614 Cl SMe Me 10.10 (bs, 1H), 7.58 (d, 1H), 7.32 (d, 1H), 4.49 (q, 2H), 2.65 (s, 3H), 2.38 (s, 3H), 1.63 (t, 3H) 5-615 Cl SO₂Me Me 11.78 (bs, 1H), 7.87 (d, 1H), 7.58 (d, 1H), 4.37 (q, 2H), 3.43 (s, 3H), 2.75 (s, 3H), 1.48 (t, 3H) 5-616 Cl SO₂Et Me 7.70 (d, 1H), 7.41 (d, 1H), 4.50 (q, 2H), 3.48 (q, 2H), 2.84 (s, 3H), 1.61 (t, 3H), 1.36 (t, 3H) 5-617 Cl SOEt Me 7.65 (d, 1H), 7.27 (d, 1H), 4.46 (q, 2H), 3.22-3.29 (m, 1H), 3.08-3.17 (m, 1H), 2.70 (s, 3H), 1.62 (t, 3H), 1.39 (t, 3H) 5-618 Cl SOMe Me 11.69 (bs, 1H), 7.74 (d, 1H), 7.45 (d, 1H), 4.35 (q, 2H), 3.02 (s, 3H), 2.72 (s, 3H), 1.47 (t, 3H) 5-619 Cl SEt Me 10.00 (bs, 1H), 7.58 (d, 1H), 7.32 (d, 1H), 5.30 (s, 3H), 4.49 (q, 2H), 2.87 (q, 2H), 2.64 (s, 3H), 1.63 (t, 3H), 1.21 (t, 3H) 5-620 Cl SMe CF₃ 5-621 Cl SMe CF₃ 5-622 Cl SOMe CF₃ 5-623 Cl SO₂Me CF₃ 11.97 (s, 1H), 8.26 (d, 1H), 8.21 (d, 1H), 4.39 (q, 2H), 3.54 (s, 3H), 1.49 (t, 3H) 5-624 Cl CF₃ Cl 5-625 Cl CH₂(4-methyl-1,2,4- Cl 11.77 (brs, 1H), 7.86 (s, 1H), 7.74 triazolin-5-on-1-yl) (d, 1H), 7.68 (d, 1H), 5.14 (s, 2H), 4.35 (q, 2H), 3.18 (s, 3H), 1.46 (t, 3H) 5-626 Cl CH₂(4-methyl-3- Cl 11.80 (brs, 1H), 7.74 (d, 1H), 7.68 isopropoxy-1,2,4- (d, 1H), 5.09 (s, 2H), 4.73 (m, 1H), triazolin-5-on-1-yl) 4.35 (q, 2H), 2.99 (s, 3H), 1.47 (t, 3H), 1.27 (d, 6H) 5-627 Cl CH₂(4-methyl-3- Cl 11.80 (brs, 1H), 7.75 (d, 1H), 7.68 trifluoroethoxy-1,2,4- (d, 1H), 5.12 (s, 2H), 4.85 (q, 2H), 4.36 triazolin-5-on-1-yl) (q, 2H), 3.07 (s, 3H), 1.51 (t, 3H) 5-628 Cl NHAc Cl 11.80 (brs, 1H), 9.99 (brs, 1H), 7.71 (d, 1H), 7.68 (d, 1H), 4.36 (q, 2H), 2.10 (s, 3H), 1.46 (t, 3H) 5-629 Cl OMe Cl 11.71 (bs, 1H), 7.68 (d, 1H), 7.54 (d, 1H), 4.36 (q, 2H), 3.88 (s, 3H), 1.47 (t, 3H) 5-630 Cl OEt Cl 11.72 (bs, 1H), 7.67 (d, 1H), 7.51 (d, 1H), 4.35 (q, 2H), 4.11 (q, 2H), 1.47 (t, 3H), 1.39 (t, 3H) 5-631 Cl O(CH₂)₃OMe Cl 9.57 (bs, 1H), 7.52 (d, 1H), 7.47 (d, 1H), 4.47 (q, 2H), 4.16 (t, 2H), 3.66 (t, 2H), 3.39 (s, 3H), 2.15 (quin, 2H), 1.63 (t, 3H) 5-632 Cl O(CH₂)₂SMe Cl 11.75 (bs, 1H), 7.68 (d, 1H), 7.54 (d, 1H), 4.35 (q, 2H), 4.18 (t, 2H), 2.94 (t, 2H), 2.16 (s, 3H), 1.46 (t, 3H) 5-633 Cl O(CH₂)₃SMe Cl 11.80 (bs, 1H), 7.59 (d, 1H), 7.44 (d, 1H), 4.27 (q, 2H), 4.09 (t, 2H), 2.71 (t, 2H), 2.08 (s, 3H), 2.06 (quin, 2H), 1.41 (t, 3H) 5-634 Cl O(CH₂)₂SEt Cl 11.77 (bs, 1H), 7.63 (d, 1H), 7.49 (d, 1H), 4.31 (q, 2H), 4.15 (t, 2H), 2.97 (t, 2H), 2.62 (q, 2H), 1.44 (t, 3H), 1.21 (t, 3H) 5-635 Cl cyclopropylmethoxy Cl 11.74 (bs, 1H), 7.65 (d, 1H), 7.50 (d, 1H), 4.33 (q, 2H), 3.89 (d, 2H), 1.45 (t, 3H), 1.25-1.33 (m, 1H), 0.57-0.62 (m, 2H), 0.32-0.35 (m, 2H) 5-636 Cl tetrahydrofuran-2- Cl 11.71 (bs, 1H), 7.67 (d, 1H), 7.52 (d, ylmethoxy 1H), 4.35 (q, 2H), 4.20-4.26 (m, 1H), 4.00-4.05 (m, 1H), 3.94-3.99 (m, 1H), 3.75-3.82 (m, 1H), 3.65-3.72 (m, 1H), 1.98-2.08 (m, 1H), 1.75-1.90 (m, 3H), 1.47 (t, 3H) 5-637 Cl 1,4-dioxan-2- Cl 11.75 (bs, 1H), 7.67 (d, 1H), 7.53 (d, ylmethoxy 1H), 4.35 (q, 2H), 3.97-4.06 (m, 2H), 3.90-3.95 (m, 1H), 3.98 (dd, 1H), 3.77 (dd, 1H), 3.60-3.70 (m, 2H), 3.47-3.55 (m, 2H), 1.46 (t, 3H) 5-638 Cl Cl Cl 7.48 (d, 1H), 7.44 (d, 1H), 4.40 (q, 2H), 1.58 (t, 3H) 5-639 Cl Br Cl 11.79 (s, 1H), 7.81 (d, 1H), 7.78 (d, 1H), 4.35 (q, 2H), 1.47 (t, 3H) 5-640 Cl I Cl 13.75 (brs, 1H), 7.76 (d, 1H), 7.72 (d, 1H), 4.36 (q, 2H), 1.47 (t, 3H) 5-641 Cl SEt Cl 5-642 Cl SOEt Cl 5-643 Cl SO₂Et Cl 5-644 Cl S(CH₂)₂OMe Cl 7.59 (d, 1H), 7.55 (d, 1H), 4.49 (q, 2H), 3.56 (t, 2H), 3.32 (s, 3H), 3.13 (t, 2H), 1.63 (t, 3H) 5-645 Cl SO(CH₂)₂OMe Cl 7.69 (d, 1H), 7.49 (d, 1H), 4.46 (q, 2H), 3.90 (m, 1H), 3.74 (m, 1H), 3.65 (m, 1H), 3.41-3.31 (m, 1H) 3.37 (s, 3H), 1.61 (t, 3H) 5-646 Cl SO₂(CH₂)₂OMe Cl 7.69 (d, 1H), 7.61 (d, 1H), 4.50 (q, 2H), 3.88 (t, 2H), 3.73 (t, 2H), 3.22 (s, 3H), 1.62 (t, 3H) 5-647 Cl OMe Br 11.70 (bs, 1H), 7.81 (d, 1H), 7.46 (d, 1H), 4.36 (q, 2H), 3.87 (s, 3H), 1.47 (t, 3H), 5-648 Cl OEt Br 11.73 (bs, 1H), 7.79 (d, 1H), 7.43 (d, 1H), 4.33 (q, 2H), 4.08 (q, 2H), 1.46 (t, 3H), 1.42 (t, 3H) 5-649 Cl O(CH₂)₂OMe Br 9.00 (bs, 1H), 7.64 (d, 1H), 7.45 (d, 1H), 4.46 (q, 2H), 4.25 (t, 2H), 3.84 (t, 2H), 3.49 (s, 3H), 1.63 (t, 3H) 5-650 Cl tetrahydrofuran-2- Br 11.70 (bs, 1H), 7.80 (d, 1H), 7.45 (d, ylmethoxy 1H), 4.35 (q, 2H), 4.20-4.30 (m, 1H), 4.00-4.05 (m, 1H), 3.90-3.95 (m, 1H), 3.77-3.82 (m, 1H), 3.68-3.72 (m, 1H), 2.00-2.08 (m, 1H), 1.79-1.90 (m, 3H), 1.45 (t, 3H) 5-651 Cl 1,4-dioxan-2- Br 11.71 (bs, 1H), 7.81 (d, 1H), 7.46 (d, ylmethoxy 1H), 4.35 (q, 2H), 3.88-4.08 (m, 4H), 3.75-3.81 (m, 1H), 3.60-3.70 (m, 2H), 3.45-3.55 (m, 2H), 1.47 (t, 3H) 5-652 Cl OCH₂(CO)NMe₂ Br 11.73 (bs, 1H), 7.82 (d, 1H), 7.48 (d, 1H), 4.72 (s, 2H), 4.35 (q, 2H), 3.02 (s, 3H), 2.88 (s, 3H), 1.47 (t, 3H) 5-653 Cl CH₂OCH₂iPr SO₂Me 0.92 (d, 6H), 1.64 (t, 3H), 1.90 (m, 1H), 3.28 (s, 3H), 3.43 (d, 2H), 4.50 (q, 2H), 5.12 (s, 2H), 7.78 (d, 1H), 8.16 (d, 1H), 10.42 (s, 1H) 5-654 Cl CH₂OCH₂cPr SO₂Me 0.25 (m, 2H), 0.58 (m, 2H), 1.10 (m, 1H), 1.64 (t, 3H), 3.32 (s, 3H), 3.49 (d, 2H), 4.50 (q, 2H), 5.16 (s, 2H), 7.79 (d, 1H), 8.16 (d, 1H), 10.7 (s, 1H) 5-655 Cl CH₂OC₂H₄OMe SO₂Me 1.62 (t, 3H), 3.32 (s, 3H), 3.35 (s, 3H), 3.58 (m, 2H), 3.79 (m, 2H), 4.48 (q, 2H), 5.16 (s, 2H), 7.78 (d, 1H), 8.11 (d, 1H), 10.85 (s, 1H) 5-656 Cl CH₂OCH₂CF₃ SMe 7.65 (d, 1H), 7.23 (d, 1H), 4.77 (s, 2H), 4.49 (q, 2H), 4.14 (q, 2H), 2.5 (s, 3H), 1.49 (t, 3H) 5-657 Cl pyrazol-1-yl SO₂Me 5-658 Cl 4-Me-pyrazol-1-yl SO₂Me 12.00 (bs, 1H), 8.14 (s, 1H), 8.08 (d, 1H), 7.78 (s, 1H), 7.69 (s, 1H), 4.30 (q, 2H), 3.16 (s, 3H), 2.12 (s, 3H), 1.41 (t, 3H) 5-659 Cl 4-MeO-pyrazol-1-yl SO₂Me 5-660 Cl 4-CN-pyrazol-1-yl SO₂Me 5-661 Cl 4-Cl-pyrazol-1-yl SO₂Me 5-662 Cl 3,5-Me₂-pyrazol-1-y1 SO₂Me 5-663 Cl 1,2,4-triazol-1-yl SO₂Me 5-664 Cl 5-iPr-1,2,4-triazol-1- SO₂Me 12.02 (s, 1H), 8.78 (s, 1H), 8.25 (bs, yl 2H), 4.37 (q, 2H), 3.28 (s, 3H), 3.09 (m, 1H), 1.47 (t, 3H), 1.30 (d, 6H) 5-665 Cl 5-EtS-1,2,4-triazol- SO₂Me 12.04 (s, 1H), 8.95 (s, 1H), 8.28 (d, 1-yl 1H), 8.26 (d, 1H), 4.37 (q, 2H), 3.29 (s, 3H), 3.12 (q, 2H), 1.47 (t, 3H), 1.34 (t, 3H) 5-666 Cl OPr SO₂Me 10.10 (bs, 1H), 8.04 (d, 1H), 7.60 (d, 1H), 4.50 (q, 2H), 4.26 (t, 2H), 3.30 (s, 3H), 1.97 (quin, 2H), 1.64 (t, 2H), 1.10 (t, 3H) 5-667 Cl OPr SO₂Et 9.77 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.50 (q, 2H), 4.24 (t, 2H), 3.46 (q, 2H), 1.96 (quin, 2H), 1.64 (t, 3H), 1.29 (t, 3H), 1.09 (t, 3H) 5-668 Cl isobutoxy SO₂Me 10.35 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.50 (q, 2H), 4.08 (d, 2H), 3.30 (s, 3H), 2.28 (sep, 1H), 1.62 (t, 3H), 1.11 (s, 3H), 1.09 (s, 3H), 5-669 Cl butoxy SO₂Me 10.40 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.50 (q, 2H), 4.29 (t, 2H), 3.29 (s, 3H), 1.89-1.96 (m, 2H), 1.64 (t, 3H), 1.51-1.60 (m, 2H), 1.02 (t, 3H) 5-670 Cl cyclopropylmethoxy SO₂Me 10.60 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.51 (q, 2H), 4.13 (d, 2H), 3.35 (s, 3H), 1.64 (t, 3H), 1.43-1.49 (m, 1H), 0.68-0.71 (m, 2H), 0.47-0.50 (m, 2H) 5-671 Cl cyclopropylmethoxy SO₂Et 10.25 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.51 (q, 2H), 4.12 (d, 2H), 3.54 (q, 2H), 1.64 (t, 3H), 1.45-1.47 (m, 1H), 1.28 (t, 3H), 0.67-0.70 (m, 2H), 0.46-0.49 (m, 2H) 5-672 Cl cyclobutylmethoxy SO₂Me 10.15 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.50 (q, 2H), 4.28 (d, 2H), 3.29 (s, 3H), 3.93-3.98 (m, 1H), 2.16-2.21 (m, 2H), 1.95-2.03 (m, 4H), 1.64 (t, 3H) 5-673 Cl cyclobutylmethoxy SO₂Et 10.37 (bs, 1H), 8.01 (d, 1H), 7.59 (d, 1H), 4.50 (q, 2H), 4.26 (d, 2H), 3.45 (q, 2H), 2.92-2.96 (m, 1H), 2.14-2.21 (m, 2H), 1.95-2.04 (m, 4H), 1.63 (t, 3H), 1.27 (t, 3H) 5-674 Cl allyloxy SO₂Me 11.92 (bs, 1H), 7.96 (d, 1H), 7.79 (d, 1H), 6.19 (m, 1H), 5.02 (d, 1H), 5.37 (d, 1H), 4.60-4.62 (m, 2H), 4.38 (q, 2H), 3.39 (s, 3H), 1.48 (t, 3H) 5-675 Cl allyloxy SO₂Et 11.92 (bs, 1H), 7.95 (d, 1H), 7.79 (d, 1H), 6.19 (m, 1H), 5.51 (d, 1H), 5.35 (d, 1H), 4.69-4.72 (m, 2H), 4.38 (q, 2H), 3.52 (q, 2H), 1.48 (t, 3H), 1.12 (t, 3H) 5-676 Cl propargyloxy SO₂Me 10.70 (bs, 1H), 8.04 (d, 1H), 7.65 (d, 1H), 4.99 (d, 2H), 4.51 (q, 2H), 3.34 (s, 3H), 2.68 (t, 1H), 1.63 (t, 3H) 5-677 Cl propargyloxy SO₂Et 10.70 (bs, 1H), 8.02 (d, 1H), 7.65 (d, 1H), 4.97 (d, 2H), 4.51 (q, 2H), 3.50 (q, 2H), 2.67 (t, 1H), 1.63 (t, 3H), 1.29 (t, 3H) 5-678 Cl OCH₂CN SO₂Et 11.30 (bs, 1H), 8.02 (d, 1H), 7.71 (d, 1H), 5.08 (s, 2H), 5.52 (q, 2H), 3.45 (q, 2H), 1.58 (t, 3H), 1.33 (t, 3H) 5-679 Cl OCH₂CH₂F SO₂Me 11.15 (bs, 1H), 8.06 (d, 1H), 7.65 (d, 1H), 4.91 (bs, 1H), 4.83 (bs, 1H), 4.62 (bs, 1H), 4.57 (bs, 1H), 4.52 (q, 2H), 3.34 (s, 3H), 1.63 (t, 3H) 5-680 Cl OCH₂CH₂F SO₂Et 8.04 (d, 1H), 7.71 (d, 1H), 4.91-4.93 (m, 1H), 4.79-4.82 (m, 1H), 4.58-4.59 (m, 1H), 4.50-4.52 (m, 1H), 4.46 (q, 2H), 3.55 (q, 2H), 1.61 (t, 3H), 1.25 (t, 3H) 5-681 Cl OCH₂CF₃ SO₂Me 5-682 Cl OCH₂CF₃ SO₂Et 11.00 (bs, 1H), 8.05 (d, 1H), 7.70 (d, 1H), 4.72 (q, 2H), 4.52 (q, 2H), 3.48 (q, 2H), 1.63 (t, 3H), 1.30 (t, 3H) 5-683 Cl O(CH₂)₂OEt SO₂Et 10.56 (bs, 1H), 8.03 (d, 1H), 7.62 (d, 1H), 4.50 (q, 2H), 4.47 (t, 2H), 3.90 (t, 2H), 3.64 (q, 2H), 3.55 (q, 2H), 1.64 (t, 3H), 1.27 (t, 3H), 1.27 (t, 3H) 5-684 Cl O(CH₂)₂SMe SO₂Me 10.70 (bs, 1H), 8.05 (d, 1H), 7.64 (d, 1H), 4.51 (q, 2H), 4.45 (t, 2H), 3.35 (s, 3H), 3.04 (t, 2H), 2.23 (s, 3H), 1.64 (t, 3H) 5-685 Cl O(CH₂)₂SMe SO₂Et 10.60 (bs, 1H), 8.03 (d, 1H), 7.63 (d, 1H), 4.51 (q, 2H), 4.44 (t, 2H), 3.53 (q, 2H), 3.02 (t, 2H), 2.22 (s, 3H), 1.64 (t, 3H), 1.28 (t, 3H) 5-686 Cl O(CH₂)₃SMe SO₂Me 10.56 (bs, 1H), 8.04 (d, 1H), 7.62 (d, 1H), 4.51 (q, 2H), 4.39 (t, 2H), 3.29 (s, 3H), 2.75 (t, 2H), 2.23 (quin, 2H), 2.16 (s, 3H), 1.64 (t, 3H) 5-687 Cl O(CH₂)₃SMe SO₂Et 10.55 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.51 (q, 2H), 4.37 (t, 2H), 3.45 (q, 2H), 2.75 (t, 2H), 2.22 (quin, 2H), 2.16 (s, 3H), 1.64 (t, 3H), 1.28 (t, 3H) 5-688 Cl O(CH₂)₂SEt SO₂Me 10.66 (bs, 1H), 8.05 (d, 1H), 7.63 (d, 1H), 4.51 (q, 2H), 4.43 (t, 2H), 3.35 (s, 3H), 3.07 (t, 2H), 2.67 (q, 2H), 1.64 (t, 3H), 1.31 (t, 3H) 5-689 Cl O(CH₂)₂SEt SO₂Et 10.60 (bs, 1H), 8.03 (d, 1H), 7.62 (d, 1H), 4.51 (q, 2H), 4.42 (t, 2H), 3.52 (q, 2H), 3.06 (t, 2H), 2.66 (q, 2H), 1.64 (t, 3H), 1.31 (t, 3H), 1.30 (t, 3H) 5-690 Cl 1,3-dioxolan-2- SO₂Me 9.90 (bs, 1H), 8.05 (d, 1H), 7.65 (d, ylmethoxy 1H), 5.50 (t, 1H), 4.49 (q, 2H), 4.31 (d, 2H), 4.07-4.10 (m, 2H), 3.98-4.02 (m, 2H), 3.37 (s, 3H), 1.64 (t, 3H) 5-691 Cl 3-(1H-tetrazol-1- SO₂Et 11.00 (bs, 1H), 8.81 (s, 1H), 8.00 (d, yl)propoxy 1H), 7.62 (d, 1H), 4.76 (t, 2H), 4.50 (q, 2H), 4.36 (t, 2H), 3.35 (q, 2H), 2.59 (quin, 2H), 1.63 (t, 3H), 1.27 (t, 3H) 5-692 Cl 3-(2H-tetrazol-2- SO₂Et 10.50 (bs, 1H), 8.53 (s, 1H), 8.02 (d, yl)propoxy 1H), 7.63 (d, 1H), 4.97 (t, 2H), 4.50 (q, 2H), 4.39 (t, 2H), 3.42 (q, 2H), 2.68 (quin, 2H), 1.63 (t, 3H), 1.30 (t, 3H) 5-693 Cl tetrahydro-2H- SO₂Et 10.50 (bs, 1H), 8.01 (d, 1H), 7.60 (d, pyran-2-ylmethoxy 1H), 4.50 (q, 2H), 4.40 (dd, 1H), 4.06-4.13 (m, 2H), 3.87-3.93 (m, 1H), 3.47-3.59 (m, 3H), 1.89-1.93 (m, 1H), 1.61-1.68 (m, 4H), 1.61 (t, 3H), 1.26 (t, 3H) 5-694 Cl tetrahydro-2H- SO₂Me 10.05 (bs, 1H), 8.04 (d, 1H), 7.61 (d, pyran-2-ylmethoxy 1H), 4.49 (q, 2H), 4.41 (dd, 1H), 4.14 (dd, 1H), 4.09 (dt, 1H), 3.89-3.94 (m, 1H), 3.51-3.57 (m, 1H), 3.35 (s, 3H), 1.91-1.94 (m, 1H), 1.61 (t, 3H), 1.55- 1.68 (m, 4H), 1.42-1.45 (m, 1H) 5-695 Cl tetrahydrofuran-3- SO₂Me 10.70 (bs, 1H), 8.04 (d, 1H), 7.61 (d, ylmethoxy 1H), 4.51 (q, 2H), 4.28 (d, 2H), 3.91- 4.00 (m, 2H), 3.79-3.88 (m, 2H), 3.29 (s, 3H), 2.88-2.94 (m, 1H), 2.11-2.17 (m, 1H), 1.80-1.90 (m, 1H), 1.63 (t, 3H) 5-696 Cl tetrahydrofuran-3- SO₂Et 10.70 (bs, 1H), 8.02 (d, 1H), 7.60 (d, ylmethoxy 1H), 4.51 (q, 2H), 4.26 (d, 2H), 3.90- 3.99 (m, 2H), 3.78-3.86 (m, 2H), 3.43 (q, 2H), 2.86-2.93 (m, 1H), 2.10-2.18 (m, 1H), 1.80-1.89 (m, 1H), 1.65 (t, 3H), 1.29 (t, 3H) 5-697 Cl F SOMe 7.82 (dd, 1H), 7.73 (d, 1H), 4.48 (q, 2H), 2.91 (s, 3H), 1.62 (t, 3H) 5-698 Cl F SO₂Me 8.02 (dd, 1H), 7.71 (d, 1H), 4.50 (q, 2H), 3.31 (s, 3H), 1.63 (t, 3H) 5-699 Cl SO₂Me SO₂Me 11.99 (s, 1H), 8.38 (d, 1H), 8.31 (d, 1H), 4.39 (q, 2H), 3.67 (s, 3H), 3.58 (s, 3H), 1.48 (t, 3H) 5-700 Cl S(CH₂)₂OMe SO₂Me 5-701 Cl SO(CH₂)₂OMe SO₂Me 5-702 Cl SO₂(CH₂)₂OMe SO₂Me 5-703 Cl SEt SO₂Me 5-704 Cl SOEt SO₂Me 5-705 Cl SO₂Et SO₂Me 5-706 Br SO₂Me Me 9.69 (bs, 1H), 7.59 (d, 1H), 7.43 (d, 1H), 4.53 (q, 2H), 3.34 (s, 3H), 2.86 (s, 3H), 1.65 (t, 3H) 5-707 Br SOMe Me 7.55 (d, 1H), 7.32 (d, 1H), 4.48 (q, 2H), 2.96 (s, 3H), 2.73 (s, 3H), 1.64 (t, 3H) 5-708 Br SO₂Et Me 9.29 (bs, 1H), 7.59 (d, 1H), 7.47 (d, 1H), 4.52 (q, 2H), 3.49 (q, 2H), 2.85 (s, 3H), 1.65 (t, 3H), 1.37 (t, 3H) 5-709 Br SOEt Me 10.19 (bs, 1H), 7.52-7.56 (m, 1H), 7.29-7.33 (m, 1H), 4.46 (q, 2H), 3.18- 3.25 (m, 1H), 3.05-3.15 (m, 1H), 2.70 (s, 3H), 1.64 (t, 3H), 1.41 (t, 3H) 5-710 Br SEt Me 10.00 (bs, 1H), 7.46 (d, 1H), 7.35 (d, 1H), 4.52 (q, 2H), 2.87 (q, 2H), 2.67 (s, 3H), 1.64 (t, 3H), 1.24 (t, 3H) 5-711 Br SMe Me 10.30 (bs, 1H), 7.46 (d, 1H), 7.34 (d, 1H), 4.52 (q, 2H), 2.68 (s, 3H), 2.37 (s, 3H), 1.64 (t, 3H) 5-712 Br OEt Br 11.74 (bs, 1H), 7.81 (d, 1H), 7.38 (d, 1H), 4.36 (q, 2H), 4.06 (q, 2H), 1.46 (t, 3H), 1.43 (t, 3H) 5-713 Br OCH₂(CO)NMe₂ Br 11.72 (bs, 1H), 7.85 (d, 1H), 7.44 (d, 1H), 4.69 (s, 2H), 4.37 (q, 2H), 3.20 (s, 3H), 2.88 (s, 3H), 1.48 (t, 3H) 5-714 Br O(CH₂)₃OMe Br 7.65 (d, 1H), 7.20 (d, 1H), 4.34 (q, 2H), 4.05 (t, 2H), 3.58 (t, 2H), 3.27 (s, 3H), 2.04 (quin, 2H), 1.48 (t, 3H) 5-715 Br O(CH₂)₃SMe Br 11.79 (bs, 1H), 7.77 (d, 1H), 7.34 (d, 1H), 4.31 (q, 2H), 4.07 (t, 2H), 2.73 (t, 2H), 2.09 (s, 3H), 2.08 (quin, 2H), 1.43 (t, 3H) 5-716 Br O(CH₂)₂SEt Br 11.76 (bs, 1H), 7.78 (d, 1H), 7.45 (d, 1H), 4.31 (q, 2H), 4.12 (t, 2H), 2.99 (t, 2H), 2.64 (q, 2H), 1.43 (t, 3H), 1.22 (t, 3H) 5-717 Br O(CH₂)₂SMe Br 11.73 (bs, 1H), 7.80 (d, 1H), 7.37 (d, 1H), 4.32 (q, 2H), 4.15 (t, 2H), 2.96 (t, 2H), 2.17 (s, 3H), 1.44 (t, 3H) 5-718 Br 1,4-dioxan-2- Br 11.70 (bs, 1H), 7.84 (d, 1H), 7.42 (d, ylmethoxy 1H), 4.37 (q, 2H), 3.90-4.06 (m, 4H), 3.77-3.82 (m, 1H), 3.60-3.70 (m, 2H), 3.50-3.56 (m, 2H), 1.47 (t, 3H) 5-719 Br tetrahydrofuran-2- Br 11.69 (bs, 1H), 7.84 (d, 1H), 7.41 (d, ylmethoxy 1H), 4.37 (q, 2H), 4.25-4.32 (m, 1H), 4.00-4.05 (m, 1H), 4.89-4.93 (m, 1H), 4.79-4.85 (m, 1H), 4.67-4.73 (m, 1H), 2.00-2.10 (m, 1H), 1.80-1.95 (m, 3H), 1.47 (t, 3H) 5-720 Br OMe I 11.67 (bs, 1H), 8.00 (d, 1H), 7.23 (d, 1H), 4.37 (q, 2H), 3.83 (s, 3H), 1.47 (t, 3H) 5-721 Br OEt I 11.70 (bs, 1H), 7.90 (d, 1H), 7.12 (d, 1H), 4.28 (q, 2H), 4.01 (q, 2H), 1.44 (t, 3H), 1.41 (t, 3H) 5-722 Br O(CH₂)₂OMe 1 10.21 (bs, 1H), 7.91 (d, 1H), 7.17 (d, 1H), 4.50 (q, 2H), 4.23 (t, 2H), 3.89 (t, 2H), 3.50 (s, 3H), 1.63 (t, 3H) 5-723 Br O(CH₂)₃OMe I 11.10 (bs, 1H), 7.88 (d, 1H), 7.14 (d, 1H), 4.49 (q, 2H), 4.12 (t, 2H), 3.67 (t, 2H), 3.39 (s, 3H), 2.17 (quin, 2H), 1.62 (t, 3H) 5-724 Br O(CH₂)₂SMe I 11.70 (bs, 1H), 7.93 (d, 1H), 7.15 (d, 1H), 4.29 (q, 2H), 4.11 (t, 2H), 2.98 (t, 2H), 2.19 (s, 3H), 1.42 (t, 3H) 5-725 Br O(CH₂)₂SEt I 11.80 (bs, 1H), 7.89 (d, 1H), 7.12 (d, 1H), 4.26 (q, 2H), 4.08 (t, 2H), 3.01 (t, 2H), 2.65 (q, 2H), 1.40 (t, 3H), 1.23 (t, 3H) 5-726 Br O(CH₂)₃SMe I 11.80 (bs, 1H), 7.92 (d, 1H), 7.14 (d, 1H), 4.29 (q, 2H), 4.04 (t, 2H), 2.74 (t, 2H), 2.10 (s, 3H), 2.09 (quin, 2H), 1.42 (t, 3H) 5-727 Br 1,4-dioxan-2- I 11.67 (bs, 1H), 8.00 (d, 1H), 7.23 (d, ylmethoxy 1H), 4.36 (q, 2H), 3.96-4.03 (m, 2H), 3.88-3.95 (m, 2H), 3.77-3.82 (m, 1H), 3.60-3.70 (m, 2H), 3.49-3.58 (m, 2H), 1.47 (t, 3H) 5-728 Br tetrahydrofuran-2- I 11.67 (bs, 1H), 8.00 (d, 1H), 7.22 (d, ylmethoxy 1H), 4.36 (q, 2H), 4.25-4.35 (m, 1H), 3.95-4.01 (m, 1H), 3.80-3.90 (m, 2H), 3.68-3.75 (m, 1H), 2.00-2.10 (m, 1H), 1.80-1.95 (m, 3H), 1.47 (t, 3H) 5-729 Br OMe SMe 11.55 (bs, 1H), 7.79 (d, 1H), 7.32 (d, 1H), 4.40 (q, 2H), 3.90 (s, 3H), 2.41 (s, 3H), 1.48 (t, 3H) 5-730 Br OMe SO₂Me 10.70 (bs, 1H), 7.93 (d, 1H), 7.29 (d, 1H), 4.57 (q, 2H), 4.10 (s, 3H), 3.30 (s, 3H), 1.64 (t, 3H) 5-731 I SMe Me 9.31 (bs, 1H), 7.37 (d, 1H), 7.35 (d, 1H), 4.57 (q, 2H), 2.73 (s, 3H), 2.34 (s, 3H), 1.67 (t, 3H) 5-732 I SOMe Me 11.62 (bs, 1H), 7.56 (d, 1H), 7.48 (d, 1H), 4.41 (q, 2H), 2.94 (s, 3H), 2.73 (s, 3H), 1.48 (t, 3H) 5-733 I SO₂Et Me 9.20 (bs, 1H), 7.47 (s, 2H), 4.57 (q, 2H), 3.43-3.49 (m, 2H), 2.86 (s, 3H), 1.67 (t, 3H), 1.45 (t, 3H) 5-734 I SOEt Me 7.44 (d, 1H), 7.32 (d, 1H), 4.52 (q, 2H), 3.12-3.19 (m, 1H), 3.02-3.09 (m, 1H), 2.66 (s, 3H), 1.65 (t, 3H), 1.44 (t, 3H) 5-735 I SEt Me 10.04 (bs, 1H), 7.35 (s, 2H), 4.56 (q, 2H), 2.85 (q, 2H), 2.71 (s, 3H), 1.65 (t, 3H), 1.25 (t, 3H) 5-736 I O(CH₂)₃OMe SO₂Et 10.20 (bs, 1H), 8.10 (d, 1H), 7.48 (d, 1H), 4.56 (q, 2H), 4.35 (t, 2H), 3.64 (t, 2H), 3.45 (q, 2H), 3.39 (s, 3H), 2.23 (quin, 2H), 1.67 (t, 3H), 1.27 (t, 3H) 5-737 OH SMe CHF₂ 8.28 (d, 1H), 7.38 (m, 1H), 7.22 (t, 1H), 4.43 (q, 2H), 2.39 (s, 3H), 1.63 (t, 3H) 5-738 OH SO₂Me CHF₂ 5-739 OH SOMe CHF₂ 5-740 OH SO₂Me CF₃ 8.10 (d, 1H), 6.83 (d, 1H), 4.31 (q, 2H), 3.41 (s, 3H), 1.44 (t, 3H) 5-741 OH SCH₂Ph CF₃ 5-742 OMe SMe CHF₂ 8.22 (d, 1H), 7.65 (d, 1H), 7.23 (t, 1H), 4.45 (q, 2H), 4.18 (s, 3H), 2.47 (s, 3H), 1.62 (t, 3H) 5-743 OMe SO₂Me CHF₂ 5-744 OMe SOMe CHF₂ 5-745 OMe SEt CF₃ 5-746 OMe SMe OMe 5-747 OMe SOMe OMe 5-748 OMe SO₂Me OMe 5-749 OMe SMe F 5-750 OMe SOMe F 5-751 OMe SO₂Me F 5-752 OEt SMe CF₃ 5-753 OEt SOMe CF₃ 5-754 OEt SO₂Me CF₃ 5-755 OEt SEt CF₃ 5-756 OEt SOEt CF₃ 5-757 OEt SO₂Et CF₃ 5-758 OEt S(CH₂)₂OMe CF₃ 5-759 OEt SO(CH₂)₂OMe CF₃ 5-760 OEt SO₂(CH₂)₂OMe CF₃ 5-761 OEt SMe Cl 1.60 (t, 3H), 1.62 (t, 3H), 2.51 (s, 3H), 4.37 (q, 2H), 4.44 (q, 2H), 7.43 (d, 1H), 8.03 (d, 1H), 10.50 (s, 1H) 5-762 OEt SOMe Cl 5-763 OEt SO₂Me Cl 5-764 OEt SEt Cl 5-765 OEt SOEt Cl 5-766 OEt SO₂Et Cl 5-767 OEt S(CH₂)₂OMe Cl 5-768 OEt SO(CH₂)₂OMe Cl 5-769 OEt SO₂(CH₂)₂OMe Cl 5-770 OSO₂Me SMe CF₃ 5-771 OSO₂Me SOMe CF₃ 5-772 OSO₂Me SO₂Me CF₃ 5-773 OSO₂Et SMe CF₃ 5-774 OSO₂Et SOMe CF₃ 5-775 OSO₂Et SO₂Me CF₃ 5-776 OSO₂CF₃ SMe CF₃ 5-777 OSO₂CF₃ SOMe CF₃ 5-778 OSO₂CF₃ SO₂Me CF₃ 5-779 SMe SMe H 7.53 (t, 1H), 7.38 (d, 1H), 7.34 (d, 1H), 4.42 (q, 3H), 2.49 (s, 3H), 2.36 (s, 3H), 1.48 (t, 3H) 5-780 SO₂Me SO₂Me H 8.41 (d, 1H), 8.17-8.12 (m, 2H), 4.43 (q, 3H), 3.58 (s, 6H), 1.48 (t, 3H) 5-781 SO₂Me NMe₂ CF₃ 5-782 SO₂Me NHMe CF₃ 5-783 SMe OMe F 11.50 (s, 1H), 7.35-7.47 (m, 2H), 4.40 (q, 2H), 3.96 (d, 3H), 2.33 (s, 3H), 1.47 (t, 3H) 5-784 SO₂Me NMe₂ Cl 5-785 SO₂Me NHMe Cl 5-786 SO₂Me NH₂ Cl 5-787 SO₂Me NHc-Hex Cl 5-788 SMe 4- Br 10.60 (bs, 1H), 7.71 (d, 1H), 7.63 (d, (methoxybenzyl)oxy 1H), 7.54 (d, 2H), 6.96 (d, 2H), 5.05 (s, 2H), 4.47 (q, 2H), 3.85 (s, 3H), 2.52 (s, 3H), 1.63 (t, 3H) 5-789 SMe OCH₂CHF₂ Br 10.75 (s, 1H), 7.70 (d, 1H), 7.55 (d, 1H), 6.26 (tt, 1H), 4.48 (q, 2H), 4.35 (td, 2H), 2.54 (s, 3H), 1.62 (t, 3H) 5-790 SO₂Me OMe SO₂Me 5-791 SMe O(CH₂)₃OMe SMe 11.44 (s, 1H), 7.37 (d, 1H), 7.29 (d, 1H), 4.39 (q, 2H), 4.09 (t, 2H), 3.57 (t, 2H), 3.27 (s, 3H), 2.37 (s, 3H), 2.03 (quin, 2H), 1.47 (t, 3H) 5-792 SO₂Me F SO₂Me 5-793 SO₂Me SMe SO₂Me 5-794 SO₂Me SO₂Me SO₂Me 5-795 Cl Me SMe 5-796 Cl Me SO₂Et 11.86 (bs, 1H), 8.03 (d, 1H), 7.84 (d, 1H), 4.38 (q, 2H), 3.44 (q, 2H), 2.75 (s, 3H), 1.48 (t, 3H), 1.14 (t, 3H) 5-797 Me NH(CH₂)₂OCOEt SO₂Me 10.6 (bs, 1H), 7.77 (d, 1H), 7.34 (d, 1H), 5.61 (t, 1H), 4.34 (q, 2H), 4.25 (t, 2H), 3.41 (td, 2H), 3.31 (s, 3H), 3.37 (s, 3H), 2.34 (q, 2H), 1.47 (t, 3H), 1.04 (t, 3H) 5-798 Cl propargyloxy SO₂Me 5-799 Cl propargyloxy SO₂Et 5-800 Me OCH₂(CO)NMe₂ Br 5-801 F SMe Br 5-802 Br OCH₂(CO)NMe₂ I 11.70 (bs, 1H), 8.01 (d, 1H), 7.24 (d, 1H), 4.65 (s, 3H), 4.36 (q, 2H), 3.02 (s, 3H), 2.89 (s, 3H), 1.47 (t, 3H) 5-803 Cl 3-methylbutoxy SO₂Me 10.20 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.50 (q, 2H), 4.32 (t, 2H), 3.29 (s, 3H), 1.83-1.87 (m, 2H), 1.64 (t, 3H), 1.02 (s, 3H), 1.00 (s, 3H) 5-804 Cl OCH₂CH₂Cl SO₂Me 11.05 (bs, 1H), 8.05 (d, 1H), 7.64 (d, 1H), 4.58 (t, 2H), 4.51 (q, 2H), 3.99 (t, 2H), 3.35 (s, 3H), 1.63 (t, 3H) 5-805 Cl OCH₂CH₂Cl SO₂Et 10.79 (bs, 1H), 8.03 (d, 1H), 7.64 (d, 1H), 4.57 (t, 2H), 4.51 (q, 2H), 3.97 (t, 2H), 3.50 (q, 2H), 1.63 (t, 3H), 1.30 (t, 3H) 5-806 Br 2-(2-oxopyrrolidin-1- Br 11.71 (bs, 1H), 7.85 (d, 1H), 7.43 (d, yl)ethoxy 1H), 4.37 (q, 2H), 4.08 (t, 2H), 3.65 (t, 2H), 3.58 (t, 2H), 2.27 (t, 2H), 1.97 (quin, 2H), 1.48 (t, 3H) 5-807 Br 2-(2-oxo-1,3- Br 11.72 (bs, 1H), 7.86 (d, 1H), 7.43 (d, oxazolidin-3- 1H), 4.37 (q, 2H), 4.32 (t, 2H), 4.12 yl)ethoxy (t, 2H), 3.79 (t, 2H), 3.64 (t, 2H), 1.47 (t, 3H) 5-808 F SMe Cl 5-809 F SOMe Cl 5-810 F SO₂Me Cl 5-811 F SEt Cl 5-812 F SOEt Cl 5-813 F SO₂Et Cl 5-814 F SEt CF₃ 5-815 F SOEt CF₃ 5-816 F SO₂Et CF₃ 5-817 Cl SCH₂c-Pr Cl 5-818 Cl SOCH₂c-Pr Cl 5-819 Cl SO₂CH₂c-Pr Cl 5-820 Me I SO₂Me 5-821 Me I SMe 5-822 Me CN SO₂Me 5-823 Me CF₃ SO₂Me 5-824 Me pyrazol-1-yl SMe 5-825 Me 1,2,4-triazol-4-yl SO₂Me 5-826 Me COOMe SMe 5-827 Me COOMe SO₂Me

TABLE 6 Compounds of the formula (I) according to the invention in which A represents CY, B represents N and R represents phenyl

Physical data No. X Y Z (¹H-NMR, DMSO-d₆, 400 MHz) 6-1 F H Cl 6-2 F H Br 6-3 F H SO₂Me 6-4 F H SO₂Et 6-5 F H CF₃ 6-6 F H NO₂ 6-7 Cl H F 6-8 Cl H Cl 6-9 Cl H Br 6-10 Cl H SMe 6-11 Cl H SOMe 6-12 Cl H SO₂Me 7.62-7.52 (m, 8 H), 3.27 (s, 3 H) 6-13 Cl H SO₂CH₂Cl 6-14 Cl H SEt 6-15 Cl H SO₂Et 6-16 Cl H CF₃ 6-17 Cl H NO₂ 6-18 Cl H pyrazol-1-yl 6-19 Cl H 1H-1,2,4- triazol-1-yl 6-20 Br H Cl 6-21 Br H Br 6-22 Br H SO₂Me 6-23 Br H SO₂Et 6-24 Br H CF₃ 6-25 SO₂Me H Cl 6-26 SO₂Me H Br 6-27 SO₂Me H SMe 6-28 SO₂Me H SOMe 6-29 SO₂Me H SO₂Me 6-30 SO₂Me H SO₂Et 6-31 SMe H CF₃ 11.86 (s, 1 H), 7.77 (d, 1 H), 7.70 (d, 2 H), 7.75 (d, 2 H), 7.64-7.56 (m, 5 H), 2.52 (s, 3 H) 6-32 SO₂Me H CF₃ 12.26 (s, 1 H), 8.27 (m, 2 H), 7.94 (d, 1 H), 7.75 (d, 2 H), 7.70-7.56 (m, 3 H), 3.75 (s, 3 H) 6-33 SO₂Et H Cl 6-34 SO₂Et H Br 6-35 SO₂Et H SMe 6-36 SO₂Et H SOMe 6-37 SO₂Et H SO₂Me 6-38 SO₂Et H CF₃ 6-39 NO₂ H F 6-40 NO₂ H Cl 6-41 NO₂ H Br 6-42 NO₂ H I 6-43 NO₂ H CN 6-44 NO₂ H SO₂Me 12.20 (s, 1 H), 8.62 (s, 1 H), 8.41 (dd, 1 H), 7.96 (d, 1 H), 7.72-7.61 (m, 5 H), 3.40 (s, 3 H) 6-45 NO₂ H SO₂Et 6-46 NO₂ H CF₃ 6-47 Me H Cl 6-48 Me H Br 6-49 Me H SMe 6-50 Me H SO₂Me 6-51 Me H SO₂CH₂Cl 6-52 Me H SEt 6-53 Me H SO₂Et 6-54 Me H CF₃ 6-55 CH₂SO₂Me H CF₃ 6-56 Et H Cl 6-57 Et H Br 6-58 Et H SMe 6-59 Et H SO₂Me 6-60 Et H SO₂CH₂Cl 6-61 Et H SEt 6-62 Et H SO₂Et 6-63 Et H CF₃ 6-64 CF₃ H Cl 6-65 CF₃ H Br 6-66 CF₃ H SO₂Me 6-67 CF₃ H SO₂Et 6-68 CF₃ H CF₃ 6-69 NO₂ NH₂ F 6-70 NO₂ NHMe F 6-71 NO₂ NME₂ F 6-72 NO₂ Me Cl 6-73 NO₂ NH₂ Cl 6-74 NO₂ NHMe Cl 6-75 NO₂ NME₂ Cl 6-76 NO₂ NH₂ Br 6-77 NO₂ NHMe Br 6-78 NO₂ NME₂ Br 6-79 NO₂ NH₂ CF₃ 6-80 NO₂ NME₂ CF₃ 6-81 NO₂ NH₂ SO₂Me 6-82 NO₂ NH₂ SO₂Et 6-83 NO₂ NHMe SO₂Me 6-84 NO₂ NME₂ SO₂Me 6-85 NO₂ NME₂ SO₂Et 6-86 NO₂ NH₂ 1H-1,2,4- triazol-1-yl 6-87 NO₂ NHMe 1H-1,2,4- triazol-1-yl 6-88 NO₂ NME₂ 1H-1,2,4- triazol-1-yl 6-89 Me SMe H 6-90 Me SOMe H 6-91 Me SO₂Me H 6-92 Me SEt H 6-93 Me SOEt H 6-94 Me SO₂Et H 6-95 Me S(CH₂)₂OMe H 6-96 Me SO(CH₂)₂OMe H 6-97 Me SO₂(CH₂)₂OMe H 6-98 Me F F 6-99 Me F Cl 6-100 Me SEt F 6-101 Me SOEt F 6-102 Me SO₂Et F 6-103 Me Me Cl 6-104 Me F Cl 6-105 Me Cl Cl 6-106 Me NH₂ Cl 6-107 Me NHMe Cl 6-108 Me NME₂ Cl 6-109 Me O(CH₂)₂OMe Cl 6-110 Me O(CH₂)₃OMe Cl 6-111 Me O(CH₂)₄OMe Cl 6-112 Me OCH₂CONME₂ Cl 6-113 Me O(CH₂)₂—CO—NME₂ Cl 6-114 Me O(CH₂)₂—NH(CO)NME₂ Cl 6-115 Me O(CH₂)₂—NH(CO)NHCO₂Et Cl 6-116 Me O(CH₂)₂—NHCO₂Me Cl 6-117 Me O—CH₂—NHSO₂cPr Cl 6-118 Me O(CH₂)-5-2,4-dimethyl-2,4- Cl dihydro-3H-1,2,4-triazol-3- one 6-119 Me O(CH₂)-3,5-dimethyl-1,2- Cl oxazol-4-yl 6-120 Me SMe Cl 6-121 Me SOMe Cl 6-122 Me SO₂Me Cl 6-123 Me SEt Cl 6-124 Me SOEt Cl 6-125 Me SO₂Et Cl 6-126 Me S(CH₂)₂OMe Cl 6-127 Me SO(CH₂)₂OMe Cl 6-128 Me SO₂(CH₂)₂OMe Cl 6-129 Me NH₂ Br 6-130 Me NHMe Br 6-131 Me NME₂ Br 6-132 Me O(CH₂)-(CO)NEt₂ Br 6-133 Me O(CH₂)-5-pyrrolidin-2-one Br 6-134 Me SMe Br 6-135 Me SOMe Br 6-136 Me SO₂Me Br 6-137 Me SEt Br 6-138 Me SOEt Br 6-139 Me SO₂Et Br 6-140 Me SMe I 6-141 Me SOMe I 6-142 Me SO₂Me I 6-143 Me SEt I 6-144 Me SOEt I 6-145 Me SO₂Et I 6-146 Me Cl CF₃ 6-147 Me SMe CF₃ 11.84 (s, 1 H), 7.77 (d, 1 H), 7.70- 7.60 (m, 7 H), 2.45 (s, 3 H), 2.27 (s, 3 H) 6-148 Me SOMe CF₃ 11.94 (s, 1 H), 7.85 (d, 1 H), 7.75 (d, 1 H), 7.71-7.63 (m, 5 H), 3.00 (s, 3 H), 2.62 (s, 3 H) 6-149 Me SO₂Me CF₃ 11.96 (s, 1 H), 8.02 (d, 1 H), 7.87 (d, 1 H), 7.71-7.61 (m, 5 H), 3.53 (s, 3 H), 2.46 (s, 3 H) 6-150 Me SEt CF₃ 6-151 Me SOEt CF₃ 6-152 Me SO₂Et CF₃ 6-153 Me S(CH₂)₂OMe CF₃ 6-154 Me SO(CH₂)₂OMe CF₃ 6-155 Me SO₂(CH₂)₂OMe CF₃ 6-156 Me Me SO₂Me 6-157 Me 4,5-dihydro-1,2-oxazol-3-yl SO₂Me 6-158 Me 4,5-dihydro-1,2-oxazol-3-yl SO₂Et 6-159 Me 5-cyanomethyl-4,5-dihydro- SO₂Me 1,2-oxazol-3-yl 6-160 Me 5-cyanomethyl-4,5-dihydro- SO₂Et 1,2-oxazol-3-yl 6-161 Me NH₂ SO₂Me 6-162 Me NHMe SO₂Me 6-163 Me NME₂ SO₂Me 11.81 (s, 1 H), 7.83 (d, 1 H), 7.69-7.,60 (m, 5 H), 7.50 (d, 1 H), 3.31 (s, 3 H), 2.78 (s, 6 H), 2.14 (s, 3 H) 6-164 Me NH(CH₂)₂OMe SO₂Me 6-165 Me pyrazol-1-yl SO₂Me 6-166 Me OH SO₂Me 6-167 Me OMe SO₂Me 6-168 Me OMe SO₂Et 6-169 Me OEt SO₂Me 6-170 Me OEt SO₂Et 6-171 Me OiPr SO₂Me 6-172 Me OiPr SO₂Et 6-173 Me O(CH₂)₂OMe SO₂Me 6-174 Me O(CH₂)₂OMe SO₂Et 6-175 Me O(CH₂)₃OMe SO₂Me 6-176 Me O(CH₂)₃OMe SO₂Et 6-177 Me O(CH₂)₄OMe SO₂Me 6-178 Me O(CH₂)₄OMe SO₂Et 6-179 Me O(CH₂)₂NHSO2Me SO₂Me 6-180 Me O(CH₂)₂NHSO2Me SO₂Et 6-181 Me OCH₂(CO)NME₂ SO₂Me 6-182 Me OCH₂(CO)NME₂ SO₂Et 6-183 Me [1,4]dioxan-2-ylmethoxy SO₂Me 6-184 Me [1,4]dioxan-2-ylmethoxy SO₂Et 6-185 Me O(CH₂)_(2—)O(3,5-dimethoxy- SO₂Me pyrimidin-2-yl) 6-186 Me Cl SO₂Me 11.94 (s, 1 H), 8.02 (d, 1 H), 7.71- 7.62 (m, 5 H), 3.38 (s, 3 H) 6-187 Me SMe SO₂Me 6-188 Me SOMe SO₂Me 6-189 Me SO₂Me SO₂Me 12.01 (s, 1 H), 8.24 (d, 1 H), 7.93 (d, 1 H), 7.71-7.60 (m, 5 H), 3.58 (s, 3 H), 3.53 (s, 3 H), 2.46 (s, 3 H) 6-190 Me SO₂Me SO₂Et 6-191 Me SEt SO₂Me 6-192 Me SOEt SO₂Me 6-193 Me SO₂Et SO₂Me 6-194 Me S(CH₂)₂OMe SO₂Me 6-195 Me SO(CH₂)₂OMe SO₂Me 6-196 Me SO₂(CH₂)₂OMe SO2Me 6-197 CH₂SMe OMe SO₂Me 6-198 CH₂OMe OMe SO₂Me 6-199 CH₂O(CH₂)₂OMe NH(CH₂)₂OEt SO₂Me 6-200 CH₂O(CH₂)₂OMe NH(CH₂)₃OEt SO₂Me 6-201 CH₂O(CH₂)₃OMe OMe SO₂Me 6-202 CH₂O(CH₂)₂OMe NH(CH₂)₂OMe SO₂Me 6-203 CH₂O(CH₂)₂OMe NH(CH₂)₃OMe SO₂Me 6-204 Et SMe Cl 6-205 Et SO₂Me Cl 6-206 Et SMe CF₃ 6-207 Et SO₂Me CF₃ 6-208 Et F SO₂Me 6-209 Et NH(CH₂)₂OMe SO₂Me 6-210 iPr SO₂Me CF₃ 6-211 cPr SO₂Me CF₃ 6-212 CF₃ O(CH₂)₂OMe F 6-213 CF₃ O(CH₂)₃OMe F 6-214 CF₃ OCH₂CONME₂ F 6-215 CF₃ [1,4]dioxan-2-ylmethoxy F 6-216 CF₃ O(CH₂)₂OMe Cl 6-217 CF₃ O(CH₂)₃OMe Cl 6-218 CF₃ OCH₂CONME₂ Cl 6-219 CF₃ [1,4]dioxan-2-ylmethoxy Cl 6-220 CF₃ O(CH₂)₂OMe Br 6-221 CF₃ O(CH₂)₃OMe Br 6-222 CF₃ OCH₂CONME₂ Br 6-223 CF₃ [1,4]dioxan-2-ylmethoxy Br 6-224 CF₃ O(CH₂)₂OMe I 6-225 CF₃ O(CH₂)₃OMe I 6-226 CF₃ OCH₂CONMe₂ I 6-227 CF₃ [1,4]dioxan-2-ylmethoxy I 6-228 CF₃ F SO₂Me 6-229 CF₃ F SO₂Et 6-230 CF₃ O(CH₂)₂OMe SO₂Me 6-231 CF₃ O(CH₂)₂OMe SO₂Et 6-232 CF₃ O(CH₂)₃OMe SO₂Me 6-233 CF₃ O(CH₂)₃OMe SO₂Et 6-234 CF₃ OCH₂CONMe₂ SO₂Me 6-235 CF₃ OCH₂CONMe₂ SO₂Et 6-236 CF₃ [1,4]dioxan-2-ylmethoxy SO₂Me 6-237 CF₃ [1,4]dioxan-2-ylmethoxy SO₂Et 6-238 F SMe CF₃ 12.00 (s, 1 H), 7.79-7.74 (m, 21 H), 7.75 (d, 1 H), 7.70-7.58 (m, 5 H), 2.22 (s, 3 H) 6-239 F SOMe CF₃ 6-240 Cl Me Cl 6-241 Cl OCH₂CHCH₂ Cl 6-242 Cl OCH₂CHF₂ Cl 6-243 Cl O(CH₂)₂OMe Cl 6-244 Cl OCH₂(CO)NME₂ Cl 6-245 Cl O(CH₂)-5-pyrrolidin-2-one Cl 6-246 Cl SMe Cl 6-247 Cl SOMe Cl 6-248 Cl SO₂Me Cl 6-249 Cl F SMe 6-250 Cl Cl SO₂Me 12.12 (s, 1 H), 8.12 (d, 1 H), 7.80 (d, 1 H), 7.71-7.62 (m, 5 H), 3.45 (s, 3H ) 6-251 Cl COOMe SO₂Me 6-252 Cl CONME₂ SO₂Me 6-253 Cl CONMe(OMe) SO₂Me 6-254 Cl CH₂OMe SO₂Me 6-255 Cl CH₂OMe SO₂Et 6-256 Cl CH₂OEt SO₂Me 6-257 Cl CH₂OEt SO₂Et 6-258 Cl CH₂OCH₂CHF₂ SO₂Me 6-259 Cl CH₂OCH₂CF₃ SO₂Me 8.00 (d, 1 H), 7.78 (d, 2 H), 7.71 (d, 1 H), 7.61-7.65 (m, 3 H), 5.21 (s, 2 H), 4.25 (q, 2 H), 3.09 (q, 2 H) 6-260 Cl CH₂OCH₂CF₃ SO₂Et 6-261 Cl CH₂OCH₂CF₂CHF₂ SO₂Me 6-262 Cl CH₂Ocpentyl SO₂Me 6-263 Cl CH₂PO(OMe)₂ SO₂Me 6-264 Cl 4,5-dihydro-1,2-oxazol-3-yl SMe 6-265 Cl 4,5-dihydro-1,2-oxazol-3-yl SO₂Me 6-266 Cl 4,5-dihydro-1,2-oxazol-3-yl SO₂Et 6-267 Cl 5-cyanomethyl-4,5-dihydro- SO₂Me 1,2-oxazol-3-yl 6-268 Cl 5-cyanomethyl-4,5-dihydro- SO₂Et 12.12 (s, 1 H), 8.09 (d, 1 H), 7.96 1,2-oxazol-3-yl (d, 1 H), 7.71-7.60 (m, 5 H), 5.17 (m, 1 H), 3.56 (dd, 1 H), 3.41 (q, 2 H), 3.11 (dd, 1 H), 3.02-2.95 (m, 2 H), 1.14 (t, 3 H) 6-269 Cl 5-(methoxymethyl)-4,5- SO₂Et dihydro-1,2-oxazol-3-yl 6-270 Cl 5-(methoxymethyl)-5-methyl- SO₂Et 4,5-dihydro-1,2-oxazol-3-yl 6-271 Cl CH₂O-tetrahydrofuran-3-yl SO₂Me 6-272 Cl CH₂O-tetrahydrofuran-3-yl SO₂Et 6-273 Cl CH₂OCH₂-tetrahydrofuran-2-yl SO₂Me 12.06 (s, 1 H), 8.07 (d, 1 H), 7.78 (d, 1 H), 7.71-7.60 (m, 5 H), 5.04 (dd, 2 H), 3.97-3.95 (m, 1 H), 3.74- 3.50 (m, 4 H), 3.37 (s, 3 H), 1.88- 1.75 (m, H), 1.55-1.49 (m, 1 H) 6-274 Cl CH₂OCH₂-tetrahydrofuran-2-yl SO₂Et 6-275 Cl CH₂OCH₂-tetrahydrofuran-3-yl SO₂Me 6-276 Cl CH₂OCH₂-tetrahydrofuran-3-yl SO₂Et 6-277 Cl OMe SO₂Me 6-278 Cl OMe SO₂Et 6-279 Cl OEt SO₂Me 6-280 Cl OEt SO₂Et 6-281 Cl OiPr SO₂Me 6-282 Cl OiPr SO₂Et 6-283 Cl O(CH₂)₂OMe SO₂Me 6-284 Cl O(CH₂)₄OMe SO₂Me 6-285 Cl O(CH₂)₄OMe SO₂Et 6-286 Cl O(CH₂)₃OMe SO₂Me 6-287 Cl O(CH₂)₃OMe SO₂Et 6-288 Cl O(CH₂)₂OMe SO₂Me 6-289 Cl O(CH₂)₂OMe SO₂Et 6-290 Cl [1,4]dioxan-2-ylmethoxy SO₂Me 6-291 Cl [1,4]dioxan-2-ylmethoxy SO₂Et 6-292 Cl OCH₂(CO)NME₂ SO₂Me 6-293 Cl OCH₂(CO)NME₂ SO₂Et 6-294 Cl SMe SO₂Me 12.07 (s, 1 H), 8.10 (d, 1 H), 7.79 (d, 1 H), 7.71-7.62 (m, 5 H), 3.56 (s, 3 H), 2.33 (s, 3 H) 6-295 Cl SOMe SO₂Me 6-296 Br OMe Br 6-297 Br O(CH₂)₂OMe Br 6-298 Br O(CH₂)₂OMe SO₂Me 6-299 Br O(CH₂)₂OMe SO₂Et 6-300 Br O(CH₂)₃OMe SO₂Me 6-301 Br O(CH₂)₃OMe SO₂Et 6-302 Br O(CH₂)₄OMe SO₂Me 6-303 Br O(CH₂)₄OMe SO₂Et 6-304 Br [1 ,4]dioxan-2-ylmethoxy SO₂Me 6-305 Br [1 ,4]dioxan-2-ylmethoxy SO₂Et 6-306 I O(CH₂)₂OMe SO₂Me 6-307 I O(CH₂)₂OMe SO₂Et 6-308 I O(CH₂)₃OMe SO₂Me 6-309 I O(CH₂)₃OMe SO₂Et 6-310 I O(CH₂)₄OMe SO₂Me 6-311 I O(CH₂)₄OMe SO₂Et 6-312 I [1,4]dioxan-2-ylmethoxy SO₂Me 6-313 I [1,4]dioxan-2-ylmethoxy SO₂Et 6-314 OMe SMe CF₃ 6-315 OMe SOMe CF₃ 6-316 OMe SO₂Me CF₃ 6-317 OMe SOEt CF₃ 6-318 OMe SO₂Et CF₃ 6-319 OMe S(CH₂)₂OMe CF₃ 6-320 OMe SO(CH₂)₂OMe CF₃ 6-321 OMe SO₂(CH₂)₂OMe CF₃ 6-322 OMe SMe Cl 6-323 OMe SOMe Cl 6-324 OMe SO₂Me Cl 6-325 OMe SEt Cl 6-326 OMe SOEt Cl 6-327 OMe SO2Et Cl 6-328 OMe S(CH₂)₂OMe Cl 6-329 OMe SO(CH₂)₂OMe Cl 6-330 OMe SO₂(CH₂)₂OMe Cl 6-331 OCH₂c-Pr SMe CF₃ 6-332 OCH₂c-Pr SOMe CF₃ 6-333 OCH₂c-Pr SO₂Me CF₃ 6-334 OCH₂c-Pr SEt CF₃ 6-335 OCH₂c-Pr SOEt CF₃ 6-336 OCH₂c-Pr SO₂Et CF₃ 6-337 OCH₂c-Pr S(CH₂)₂OMe CF₃ 6-338 OCH₂c-Pr SO(CH₂)₂OMe CF₃ 6-339 OCH₂c-Pr SO₂(CH₂)₂OMe CF₃ 6-340 OCH₂c-Pr SMe Cl 6-341 OCH₂c-Pr SOMe Cl 6-342 OCH₂c-Pr SO₂Me Cl 6-343 OCH₂c-Pr SEt Cl 6-344 OCH₂c-Pr SOEt Cl 6-345 OCH₂c-Pr SO₂Et Cl 6-346 OCH₂c-Pr S(CH₂)₂OMe Cl 6-347 OCH₂c-Pr SO(CH₂)₂OMe Cl 6-348 OCH₂c-Pr SO₂(CH₂)₂OMe Cl 6-349 OCH₂c-Pr SMe SO₂Me 6-350 OCH₂c-Pr SOMe SO₂Me 6-351 OCH₂c-Pr SO₂Me SO₂Me 6-352 OCH₂c-Pr SEt SO₂Me 6-353 OCH₂c-Pr SOEt SO₂Me 6-354 OCH₂c-Pr SO₂Et SO₂Me 6-355 OCH₂c-Pr S(CH₂)₂OMe SO₂Me 6-356 OCH₂c-Pr SO(CH₂)₂OMe SO₂Me 6-357 OCH₂c-Pr SO₂(CH₂)₂OMe SO₂Me 6-358 SO₂Me F CF₃ 6-359 SO₂Me NH₂ CF₃ 6-360 SO₂Me NHEt Cl 6-361 SMe SEt F 6-362 SMe SMe F 6-363 Me H F 6-364 Me H OCF₃ 6-365 Et H F 6-366 CH₂SO₂Me H Br 6-367 Cl H I 6-368 Cl H CN 6-369 Cl H NME₂ 6-370 Cl H NHAc 6-371 Cl H pyrrol-1-yl 6-372 Cl H pyrrolidin-1-yl 6-373 Cl H pyrazol-1-yl 6-374 Cl H 1,2,4-triazol- 1-yl 6-375 Cl H 4-methyl-3- trifluoromethyl- 1,2,4-triazolin- 5-on-1-yl 6-376 Cl H SOMe 6-377 Br H F 6-378 Br H SMe 6-379 NHSO₂Me H CF₃ 6-380 NHSO₂Et H CF₃ 6-381 NHSO₂CF₃ H CF₃ 6-382 NHSO₂Me H SO₂Me 6-383 NHSO₂Et H SO₂Me 6-384 NHSO₂CF₃ H SO₂Me 6-385 NMeSO₂Me H CF₃ 6-386 NMeSO₂Et H CF₃ 6-387 NMeSO₂CF₃ H CF₃ 6-388 NMeSO₂Me H SO₂Me 6-389 NMeSO₂Et H SO₂Me 6-390 NMeSO₂CF₃ H SO₂Me 6-391 OMe H SO₂Me 6-392 OSO₂Me H CF₃ 6-393 OSO₂Et H CF₃ 6-394 OSO₂CF₃ H CF₃ 6-395 OSO₂Me H SO₂Me 6-396 OSO₂Et H SO₂Me 6-397 OSO₂CF₃ H SO₂Me 6-398 SMe H CF₃ 6-399 SOMe H CF₃ 6-400 SMe H F 6-401 SMe H Cl 6-402 SMe H Br 6-403 SMe H SMe 6-404 SO₂Me H SO₂Me 6-405 SO₂NMePh H Cl 6-406 SO₂NME₂ H CF₃ 6-407 Me OMe CF₃ 6-408 Me SMe CN 6-409 Me SOMe CN 6-410 Me SO₂Me CN 6-411 Me Me Cl 6-412 Me O(CH₂)₂N(Me)SO₂Me Cl 6-413 Me O(CH₂)₃SMe Br 6-414 Me O(CH₂)₂SEt Br 6-415 Me O(CH₂)₂SMe Br 6-416 Me O(CH₂)₃SMe Cl 6-417 Me O(CH₂)₂SEt Cl 6-418 Me O(CH₂)₂SMe Cl 6-419 Me OEt Cl 6-420 Me OMe Cl 6-421 Me tetrahydrofuran-2-ylmethoxy Cl 6-422 Me 1,4-dioxan-2-ylmethoxy Cl 6-423 Me OEt Cl 6-424 Me OMe Cl 6-425 Me OMe Br 6-426 Me OEt Br 6-427 Me O(CH₂)₂OMe Br 6-428 Me O(CH₂)₃OMe Br 6-429 Me tetrahydrofuran-2-ylmethoxy Br 6-430 Me 1,4-dioxan-2-ylmethoxy Br 6-431 Me SMe NME₂ 6-432 Me SOMe NME₂ 6-433 Me SO₂Me NME₂ 6-434 Me SMe imidazol-1-yl 6-435 Me SMe 1,2,4-triazol- 1-yl 6-436 Me SO₂Me imidazol-1-yl 6-437 Me SOMe 1,2,4-triazol- 1-yl 6-438 Me SO₂Me 1,2 ,4-triazol- 1-yl 6-439 Me SMe OMe 6-440 Me SOMe OMe 6-441 Me SO₂Me OMe 6-442 Me SEt OMe 6-443 Me SOEt OMe 6-444 Me SO₂Et OMe 6-445 Me SMe OEt 6-446 Me SOMe OEt 6-447 Me SO₂Me OEt 6-448 Me Me SMe 6-449 Me Me SO₂Me 6-450 Me Me SEt 6-451 Me Me SO₂Et 6-452 Me NHiPr SO₂Me 6-453 Me NHCH₂-tetrahydrofuran-2-yl SO₂Me 6-454 Me NHCH₂CONHEt SO₂Me 6-455 Me NH(CH₂)₂OEt SO₂Me 6-456 Me NHEt SO₂Me 6-457 Me NHnPr SO₂Me 6-458 Me NHCH₂iPr SO₂Me 6-459 Me NHCH₂cPr SO₂Me 6-460 Me NHCH₂CH(OMe)CH₂OMe SO₂Me 6-461 Me NHCH₂CH₂CH₂OCOMe SO₂Me 6-462 Me NHCH₂CH₂(1,3-dioxan-2-yl) SO₂Me 6-463 Me NHCH₂Ph SO₂Me 6-464 Me N(CH₃)CH₂cPr SO₂Me 6-465 Me NHCH(CH₃)CH₂OMe SO₂Me 6-466 Me NHCH(CH₃)CH₂OEt SO₂Me 6-467 Me NHCH₂CH(OMe)₂ SO₂Me 6-468 Me NHCH₂CH(Me)(OMe) SO₂Me 6-469 Me NHCH₂(1,3-dioxan-2-yl) SO₂Me 6-470 Me 4-Me-pyrazol-1-yl SO₂Me 6-471 Me 3,5-Me₂-pyrazol-1-yl SO₂Me 6-472 Me 4-MeO-pyrazol-1-yl SO₂Me 6-473 Me 4-CN-pyrazol-1-yl SO₂Me 6-474 Me 4-Cl-pyrazol-1-yl SO₂Me 6-475 Me 1,2,3-triazol-1-yl SO₂Me 12.12 (s, 1 H), 8.51 (s, 1 H), 8.14 (d, 1 H), 8.04 (/s, 1 H), 8.03 (d, 1 H), 7.70-7.57 (m, 5 H), 3,12 (s, 3 H), 1.69 (s, 3 H) 6-476 Me 1,2,4-triazol-1-yl SO₂Me 6-477 Me 5-iPr-1,2,4-triazol-1-yl SO₂Me 6-478 Me 5-EtS-1,2,4-triazol-1-yl SO₂Me 6-479 Me O(CH₂)₂SMe SO₂Me 6-480 Me O(CH₂)₃SMe SO₂Me 6-481 Me tetrahydrofuran-2-ylmethoxy SO₂Me 6-482 Me F SMe 6-483 Me SMe SO₂Et 6-484 Me SOMe SO₂Et 6-485 Me SEt SO₂Et 6-486 Me SOEt SO₂Et 6-487 Me SO₂Et SO₂Et 6-488 Me SCH₂CF₃ SO₂Me 6-489 Me SOCH₂CF₃ SO₂Me 6-490 Me SO₂CH₂CF₃ SO₂Me 6-491 Me S(CH₂)₂OMe SO₂Et 6-492 Me SO(CH₂)₂OMe SO₂Et 6-493 Me SO₂(CH₂)₂OMe SO₂Et 6-494 Me S(4-F—Ph) SO₂Me 6-495 Me SO(4-F—Ph) SO₂Me 6-496 Me SO₂(4-F—Ph) SO₂Me 6-497 Et SEt Cl 6-498 Et SOEt Cl 6-499 Et SO₂Et Cl 6-500 Et S(CH₂)₂OMe Cl 6-501 Et SO(CH₂)₂OMe Cl 6-502 Et SO₂(CH₂)₂OMe Cl 6-503 Et SOMe Cl 6-504 Et SMe Br 6-505 Et SOMe Br 6-506 Et SO₂Me Br 6-507 Et SOMe CF₃ 6-508 Et SEt CF₃ 6-509 Et SOEt CF₃ 6-510 Et SO₂Et CF₃ 6-511 Et S(CH₂)₂OMe CF₃ 6-512 Et SO(CH₂)₂OMe CF₃ 6-513 Et SO₂(CH₂)₂OMe CF₃ 6-514 Et NHiPr SO₂Me 6-515 Et SMe SO₂Et 6-516 Et SOMe SO₂Et 6-517 Et SO₂Me SO₂Et 6-518 Et SEt SO₂Et 6-519 Et SOEt SO₂Et 6-520 Et SO₂Et SO₂Et 6-521 Et S(CH₂)₂OMe SO₂Et 6-522 Et SO(CH₂)₂OMe SO₂Et 6-523 Et SO₂(CH₂)₂OMe SO₂Et 6-524 Et SEt SO₂Me 6-525 Et SOEt SO₂Me 6-526 Et SO₂Et SO₂Me 6-527 Et S(CH₂)₂OMe SO₂Me 6-528 Et SO(CH₂)₂OMe SO₂Me 6-529 Et SO₂(CH₂)₂OMe SO₂Me 6-530 Et SMe SO₂Me 6-531 Et SOMe SO₂Me 6-532 Et SO₂Me SO₂Me 6-533 nPr SMe Cl 6-534 nPr SOMe Cl 6-535 nPr SO₂Me Cl 6-536 nPr SMe Br 6-537 nPr SOMe Br 6-538 nPr SO₂Me Br 6-539 nPr SMe CF₃ 6-540 nPr SOMe CF₃ 6-541 nPr SO₂Me CF₃ 6-542 nPr SMe SO₂Me 6-543 nPr SOMe SO₂Me 6-544 nPr SO₂Me SO₂Me 6-545 iPr SOMe CF₃ 6-546 iPr SO₂Me CF₃ 6-547 iPr SMe Cl 6-548 iPr SOMe Cl 6-549 iPr SO₂Me Cl 6-550 iPr SMe Br 6-551 iPr SOMe Br 6-552 iPr SO₂Me Br 6-553 iPr SMe SO₂Me 6-554 iPr SOMe SO₂Me 6-555 iPr SO₂Me SO₂Me 6-556 cPr SMe CF₃ 6-557 cPr SOMe CF₃ 6-558 cPr SMe Cl 6-559 cPr SOMe Cl 6-560 cPr SO₂Me Cl 6-561 cPr SMe Br 6-562 cPr SOMe Br 6-563 cPr SO₂Me Br 6-564 cPr SMe SO₂Me 6-565 cPr SOMe SO₂Me 6-566 cPr SO₂Me SO₂Me 6-567 CH₂OMe F CF₃ 6-568 CH₂OMe SMe CF₃ 6-569 CH₂OMe SOMe CF₃ 6-570 CH₂OMe SO₂Me CF₃ 6-571 CH₂OMe SEt CF₃ 6-572 CH₂OMe SOEt CF₃ 6-573 CH₂OMe SO₂Et CF₃ 6-574 CH₂OMe S(CH₂)₂OMe CF₃ 6-575 CH₂OMe SO(CH₂)₂OMe CF₃ 6-576 CH₂OMe SO₂(CH₂)₂OMe CF₃ 6-577 CH₂OMe SMe Cl 6-578 CH₂OMe SOMe Cl 6-579 CH₂OMe SO₂Me Cl 6-580 CH₂OMe SEt Cl 6-581 CH₂OMe SOEt Cl 6-582 CH₂OMe SO₂Et Cl 6-583 CH₂OMe S(CH₂)₂OMe Cl 6-584 CH₂OMe SO(CH₂)₂OMe Cl 6-585 CH₂OMe SO₂(CH₂)₂OMe Cl 6-586 CH₂OMe SMe SO₂Me 6-587 CH₂OMe SOMe SO₂Me 6-588 CH₂OMe SO₂Me SO₂Me 6-589 CH₂OMe SEt SO₂Me 6-590 CH₂OMe SOEt SO₂Me 6-591 CH₂OMe SO₂Et SO₂Me 6-592 CH₂OMe S(CH₂)₂OMe SO₂Me 6-593 CH₂OMe SO(CH₂₎₂OMe SO₂Me 6-594 CH₂OMe SO₂(CH₂)₂OMe SO₂Me 6-595 CH₂OMe SMe SO₂Et 6-596 CH₂OMe SOMe SO₂Et 6-597 CH₂OMe SO₂Me SO₂Et 6-598 CH₂OMe SEt SO₂Et 6-599 CH₂OMe SOEt SO₂Et 6-600 CH₂OMe SO₂Et SO₂Et 6-601 CH₂OMe S(CH₂)₂OMe SO₂Et 6-602 CH₂OMe SO(CH₂)₂OMe SO₂Et 6-603 CH₂OMe SO₂(CH₂)₂OMe SO₂Et 6-604 CH₂OMe Cl SO₂Me 6-605 CH₂O(CH₂)₂OEt OEt SO₂Me 6-606 CF₃ SOMe SO₂Me 6-607 CF₃ O(CH₂)₃SMe SO₂Et 6-608 CF₃ O(CH₂)₂OEt SO₂Et 6-609 CF₃ O(CH₂)₂SEt SO₂Et 6-610 CF₃ O(CH₂)₂SMe SO₂Et 6-611 CF₃ O(CH₂)₂OEt SO₂Me 6-612 CF₃ O(CH₂)₂SEt SO₂Me 6-613 CF₃ O(CH₂)₂SMe SO₂Me 6-614 CF₃ O(CH₂)₃SMe SO₂Me 6-615 CF₃ oxetan-3-yloxy SO₂Et 6-616 CF₃ 2-(2-thienyl)ethoxy SO₂Et 6-617 CF₃ 2-(1H-pyrazol-1-yl)ethoxy SO₂Et 6-618 CF₃ 1,3-dioxolan-4-ylmethoxy SO₂Et 6-619 CF₃ tetrahydro-2H-pyran-2- SO₂Et ylmethoxy 6-620 CF₃ oxetan-3-yloxy SO₂Me 6-621 CF₃ 2-(2-thienyl)ethoxy SO₂Me 6-622 CF₃ 1,3-dioxolan-4-ylmethoxy SO₂Me 6-623 CF₃ tetrahydrofuran-3-ylmethoxy SO₂Me 6-624 CF₃ tetrahydro-2H-pyran-2- SO₂Me ylmethoxy 6-625 F SO₂Me CF₃ 6-626 F SCH₂Ph CF₃ 6-627 F SMe F 6-628 F SOMe F 6-629 F SO₂Me F 6-630 Cl SO₂Me H 6-631 Cl SCF₂CF₂H H 6-632 Cl SOCF₂CF₂H H 6-633 Cl SO₂CF₂CF₂H H 6-634 Cl SMe Me 6-635 Cl SOMe Me 6-636 Cl SO₂Me Me 6-637 Cl SEt Me 6-638 Cl SOEt Me 6-639 Cl SO₂Et Me 6-640 Cl SMe CF₃ 6-641 Cl SOMe CF₃ 6-642 Cl SO₂Me CF₃ 6-643 Cl CF₃ Cl 6-644 Cl CH₂(4-methyl-3-isopropoxy- Cl 1,2,4-triazolin-5-on-1-yl) 6-645 Cl CH₂(4-methyl-3-trifluoro- Cl ethoxy-1,2,4-triazolin-5-on-1- yl) 6-646 Cl CH₂(4-methyl-3-(methyl- Cl sulfanyl)-5-oxo-4,5-dihydro- 1H-1,2,4-triazol-1-yl) 6-647 Cl CH₂(4-methyl-3-(methyl- Cl sulfanyl)-5-oxo-4,5-dihydro- 1H-1,2,4-triazol-1-yl) 6-648 Cl CH₂(3-(dimethylamino)-4- Cl methyl-5-oxo-4 ,5-dihydro- 1H-1,2,4-triazol-1-yl) 6-649 Cl CH₂(pyridin-2-yl) Cl 6-650 Cl CH₂(4-cyclopropyl-3- Cl methoxy-5-oxo-4,5-dihydro- 1H-1,2,4-triazol-1-yl) 6-651 Cl CH₂(3-methyl-6-oxopyridazin- Cl 1(6H)-yl) 6-652 Cl CH₂(6-oxopyridazin-1(6H)-yl) Cl 6-653 Cl CH₂(4-cyclopropyl-5-oxo-3- Cl (2,2,2-trifluoroethoxy)-4,5- dihydro-1H-1,2,4-triazol-1-yl) 6-654 Cl CH₂(3-methoxy-4-methyl-5- Cl oxo-4,5-dihydro-1H-1,2,4- triazol-1-yl) 6-655 Cl CH₂(3,4-dicyclopropyl-5-oxo- Cl 4,5-dihydro-1H-1,2,4-triazol- 1-yl) 6-656 Cl CH₂(3-ethoxy-4-methyl-5-oxo- Cl 4,5-dihydro-1H-1,2,4-triazol- 1-yl) 6-657 Cl NHCH₂CONHEt Cl 6-658 Cl NHCH(CH₃)CONHEt Cl 6-659 Cl NHCH₂CONHiPr Cl 6-660 Cl NHCH(Me)CONH₂ Cl 6-661 Cl NHAc Cl 6-662 Cl NHCON(Me)OMe Cl 6-663 Cl OMe Cl 6-664 Cl OEt Cl 6-665 Cl O(CH₂)₃OMe Cl 6-666 Cl O(CH₂)₃SMe Cl 6-667 Cl O(CH₂)₂SEt Cl 6-668 Cl O(CH₂)₂SMe Cl 6-669 Cl cyclopropylmethoxy Cl 6-670 Cl 1,4-dioxan-2-ylmethoxy Cl 6-671 Cl tetrahydrofuran-2-ylmethoxy Cl 6-672 Cl Br Cl 6-673 Cl SO₂Me Cl 6-674 Cl SOMe Cl 6-675 Cl SMe Cl 6-676 Cl SEt Cl 6-677 Cl SOEt Cl 6-678 Cl SO₂Et Cl 6-679 Cl S(CH₂)₂OMe Cl 6-680 Cl SO(CH₂)₂OMe Cl 6-681 Cl SO₂(CH₂)₂OMe Cl 6-682 Cl 1,4-dioxan-2-ylmethoxy Br 6-683 Cl O(CH₂)₂OMe Br 6-684 Cl tetrahydrofuran-2-ylmethoxy Br 6-685 Cl OCH₂(CO)NME₂ Br 6-686 Cl O(CH₂)₃OMe Br 6-687 Cl OMe Br 6-688 Cl OEt Br 6-689 Cl Me SMe 6-690 Cl Me SO₂Et 12.00 (s, 1 H), 7.97 (d, 1 H), 7.70- 7.60 (m, 7 H), 3.39 (q, 2 H), 2.69 (s, 3 H), 1.11 (t, 3 H) 6-691 Cl CH₂N(OMe)Et SO₂Me 6-692 Cl CH₂OC₂H₄OMe SO₂Me 6-693 Cl CH₂OC₂H₄OEt SO₂Me 6-694 Cl CH₂OCH₂iPr SO₂Me 6-695 Cl CH₂OCH₂CF₃ SMe 6-696 Cl CH₂OCH₂cPr SO₂Me 6-697 Cl CH₂-(4-methyl-1,2,4-triazolin- SO₂Me 11.99 (s, 1 H), 7.84 (s, 1 H),. 7.69- 5-on-1-yl) 7.60 (m, 5 H), 7.55 (d, 1 H), 5.08 (s, 2 H), 3.17 (s, 3 H) 6-698 Cl CO₂H SO₂Me 6-699 Cl NHnPr SO₂Me 6-700 Cl NHCH₂cPr SO₂Me 6-701 Cl NHCH₂CH₂OMe SO₂Me 6-702 Cl NHCH₂CH₂OEt SO₂Me 6-703 Cl NHCH₂CH₂CH₂OMe SO₂Me 6-704 Cl NHCH₂CH₂OCOiPr SO₂Me 6-705 Cl NHCH₂CH₂OCOcPr SO₂Me 6-706 Cl pyrazol-1-yl SO₂Me 6-707 Cl 4-Me-pyrazol-1-yl SO₂Me 6-708 Cl 4-MeO-pyrazol-1-yl SO₂Me 6-709 Cl 4-CN-pyrazol-1-yl SO₂Me 6-710 Cl 4-Cl-pyrazol-1-yl SO₂Me 6-711 Cl 3,5-Me₂-pyrazol-1-yl SO₂Me 6-712 Cl 1,2,4-triazol-1-yl SO₂Me 6-713 Cl 5-iPr-1,2,4-triazol-1-yl SO₂Me 6-714 Cl 5-EtS-1,2,4-triazol-1-yl SO₂Me 6-715 Cl OPr SO₂Me 6-716 Cl OPr SO₂Et 6-717 Cl isobutoxy SO₂Me 6-718 Cl butoxy SO₂Me 6-719 Cl isohexyloxy SO₂Me 6-720 Cl allyloxy SO₂Me 6-721 Cl allyloxy SO₂Et 6-722 Cl propargyloxy SO₂Et 6-723 Cl propargyloxy SO₂Me 6-724 Cl OCH₂CH₂F SO₂Me 6-725 Cl OCH₂CH₂F SO₂Et 6-726 Cl OCH₂CF₃ SO₂Me 6-727 Cl OCH₂CF₃ SO₂Et 6-728 Cl OCH₂CN SO₂Me 6-729 Cl OCH₂CN SO₂Et 6-730 Cl O(CH₂)₂OEt SO₂Et 6-731 Cl O(CH₂)₂OEt SO₂Me 6-732 Cl O(CH₂)₃OCF₃ SO₂Me 6-733 Cl O(CH₂)₂OCF₃ SO₂Me 6-734 Cl O(CH₂)₃OCF₃ SO₂Et 6-735 Cl O(CH₂)₂OCF₃ SO₂Et 6-736 Cl O(CH₂)₃SEt SO₂Me 6-737 Cl O(CH₂)₃SMe SO₂Et 6-738 Cl O(CH₂)₃SMe SO₂Me 6-739 Cl O(CH₂)₂SEt SO₂Et 6-740 Cl O(CH₂)₂SMe SO₂Et 6-741 Cl O(CH₂)₂SEt SO₂Me 6-742 Cl O(CH₂)₂SMe SO₂Me 6-743 Cl OCH₂(CO)OEt SO₂Et 6-744 Cl OCH₂(CO)OEt SO₂Me 6-745 Cl cyclopropylmethoxy SO₂Et 6-746 Cl cyclopropylmethoxy SO₂Me 6-747 Cl cyclobutylmethoxy SO₂Me 6-748 Cl cyclobutylmethoxy SO₂Et 6-749 Cl 1,3-dioxolan-2-ylmethoxy SO₂Me 6-750 Cl tetrahydro-2H-pyran-2- SO₂Et ylmethoxy 6-751 Cl tetrahydro-2H-pyran-2- SO₂Me ylmethoxy 6-752 Cl tetrahydrofuran-3-ylmethoxy SO₂Me 6-753 Cl tetrahydrofuran-3-ylmethoxy SO₂Et 6-754 Cl 3-(1H-tetrazol-1-yl)propoxy SO₂Et 6-755 Cl 3-(2H-tetrazol-2-yl)propoxy SO₂Et 6-756 Cl F SMe 6-757 Cl F SOMe 6-758 Cl F SO₂Me 6-759 Cl SO₂Me SO₂Me 6-760 Cl SEt SO₂Me 6-761 Cl SOEt SO₂Me 6-762 Cl SO₂Et SO₂Me 6-763 Cl S(CH₂)₂OMe SO₂Me 6-764 Cl SO(CH₂)₂OMe SO₂Me 6-765 Cl SO₂(CH₂)₂OMe SO₂Me 6-766 Br SMe Me 6-767 Br SOMe Me 6-768 Br SO₂Me Me 6-769 Br SEt Me 6-770 Br SOEt Me 6-771 Br SO₂Et Me 6-772 Br OEt Br 6-773 Br O(CH₂)₃OMe Br 6-774 Br O(CH₂)₂SMe Br 6-775 Br O(CH₂)₃SMe Br 6-776 Br O(CH₂)₂SEt Br 6-777 Br OCH₂(CO)NME₂ Br 6-778 Br 1,4-dioxan-2-ylmethoxy Br 6-779 Br tetrahydrofuran-2-ylmethoxy Br 6-780 Br OMe I 6-781 Br OEt I 6-782 Br O(CH₂)₂OMe I 6-783 Br O(CH₂)₃OMe I 6-784 Br 1,4-dioxan-2-ylmethoxy I 6-785 Br tetrahydrofuran-2-ylmethoxy I 6-786 Br OCH₂(CO)NME₂ I 6-787 Br O(CH₂)₃SMe I 6-788 Br O(CH₂)₂SEt I 6-789 Br O(CH₂)₂SMe I 6-790 Br OMe SO₂Me 6-791 Br OMe SMe 6-792 I SMe Me 6-793 I SOMe Me 6-794 I SO₂Me Me 6-795 I SEt Me 6-796 I SOEt Me 6-797 I SO₂Et Me 6-798 NO₂ SMe Me 6-799 NO₂ SOMe Me 6-800 NO₂ SO₂Me Me 6-801 NO₂ SEt Me 6-802 NO₂ SOEt Me 6-803 NO₂ SO₂Et Me 6-804 NO₂ CH₂OCH₂CF₃ Cl 6-805 NO₂ NME₂ Cl 6-806 OH SMe CHF₂ 6-807 OH SOMe CHF₂ 6-808 OH SO₂Me CHF₂ 6-809 OH SMe CF₃ 6-810 OH SO₂Me CF₃ 6-811 OH SCH₂Ph CF₃ 6-812 OMe SMe Me 6-813 OMe SOMe Me 6-814 OMe SO₂Me Me 6-815 OMe SMe CHF₂ 6-816 OMe SOMe CHF₂ 6-817 OMe SO₂Me CHF₂ 6-818 OMe SMe OMe 6-819 OMe SOMe OMe 6-820 OMe SO₂Me OMe 6-821 OMe SMe F 6-822 OMe SOMe F 6-823 OMe SO₂Me F 6-824 OMe CH₂N(SO₂Me)Et Cl 6-825 OMe NHCOMe Cl 6-826 OMe NHCOEt Cl 6-827 OMe NHCOiPr Cl 6-828 OMe NHCOcycPr Cl 6-829 OMe NHCOCHCMe₂ Cl 6-830 OMe NHCOPh Cl 6-831 OMe SO₂Me SO₂Me 6-832 OEt SMe CF₃ 6-833 OEt SOMe CF₃ 6-834 OEt SO₂Me CF₃ 6-835 OEt SEt CF₃ 6-836 OEt SOEt CF₃ 6-837 OEt SO₂Et CF₃ 6-838 OEt S(CH₂)₂OMe CF₃ 6-839 OEt SO(CH₂)₂OMe CF₃ 6-840 OEt SO₂(CH₂)₂OMe CF₃ 6-841 OEt SMe Cl 6-842 OEt SOMe Cl 6-843 OEt SO₂Me Cl 6-844 OEt SEt Cl 6-845 OEt SOEt Cl 6-846 OEt SO₂Et Cl 6-847 OEt S(CH₂)₂OMe Cl 6-848 OEt SO(CH₂)₂OMe Cl 6-849 OEt SO₂(CH₂)₂OMe Cl 6-850 OSO₂Me SMe CF₃ 6-851 OSO₂Me SOMe CF₃ 6-852 OSO₂Me SO₂Me CF₃ 6-853 OSO₂Et SMe CF₃ 6-854 OSO₂Et SOMe CF₃ 6-855 OSO₂Et SO₂Me CF₃ 6-856 OSO₂CF₃ SMe CF₃ 6-857 OSO₂CF₃ SOMe CF₃ 6-858 OSO₂CF₃ SO₂Me CF₃ 6-859 SMe SMe H 6-860 SO₂Me SO₂Me H 6-861 SO₂Me SO₂Me Me 6-862 SO₂Me NME₂ CF₃ 6-863 SO₂Me NHMe CF₃ 6-864 SO₂Me pyrazol-1-yl CF₃ 6-865 SMe OMe F 6-866 SO₂Me OMe F 6-867 SO₂Me NME₂ Cl 6-868 SO₂Me NHMe Cl 6-869 SO₂Me NH₂ Cl 6-870 SO₂Me NHc-Hex Cl 6-871 SO₂Me F Cl 12.00 (s, 1 H), 8.11 (t, 1 H), 7.73- 7.71 (d, 2 H), 7.65-7.58 (m, 3 H), 7.42 (d, 1 H), 3.41 (s, 3 H) 6-872 SMe OCH₂CHF₂ Br 6-873 SO₂Me OMe SO₂Me 6-874 SMe O(CH₂)₃OMe SMe 6-875 SO₂Me F SO₂Me 6-876 SO₂Me SMe SO₂Me 6-877 SO₂Me SO₂Me SO₂Me

TABLE 7 Compounds of the formula (I) according to the invention in which A represents CY

Physical data No. B R X Y Z (¹H-NMR, DMSO-d₆, 400 MHz) 7-1 CH nPr Cl H SO₂Me 7-2 CH iPr Cl H SO₂Me 7-3 N nPr Cl H SO₂Me 7-4 N iPr Cl H SO₂Me 7-5 N cPr Cl H SO₂Me 7-6 N allyl Cl H SO₂Me 7-7 N CH₂OMe Cl H SO₂Me 7-8 CH nPr NO₂ H SO₂Me 7-9 CH iPr NO₂ H SO₂Me 7-10 N nPr NO₂ H SO₂Me 7-11 N iPr NO₂ H SO₂Me 7-12 N cPr NO₂ H SO₂Me 7-13 N allyl NO₂ H SO₂Me 7-14 N CH₂OMe NO₂ H SO₂Me 7-15 CH nPr SO₂Me H CF₃ 7-16 CH iPr SO₂Me H CF₃ 7-17 N nPr SO₂Me H CF₃ 8.35 (d, 1H), 8.31 (s, 1H), 8.14 (d, 1H), 4.36 (t, 2H), 3.46 (s, 3H), 1.89 (m, 2H), 0.90 (t, 3H) 7-18 N iPr SO₂Me H CF₃ 7-19 N cPr SO₂Me H CF₃ 7-20 N allyl SO₂Me H CF₃ 7-21 N CH₂OMe SO₂Me H CF₃ 7-22 CH nPr Cl CH₂OCH₂CF₃ SO₂Me 7-23 CH iPr Cl CH₂OCH₂CF₃ SO₂Me 7-24 N nPr Cl CH₂OCH₂CF₃ SO₂Me 8.08 (d, 1H), 7.72 (d, 1H), 5.32 (s, 2H), 4.33 (t, 2H), 4.04 (q, 2H), 3.22 (s, 3H), 1.97 (m, 2H), 0.97 (t, 3H) 7-25 N iPr Cl CH₂OCH₂CF₃ SO₂Me 7-26 N cPr Cl CH₂OCH₂CF₃ SO₂Me 7-27 N allyl Cl CH₂OCH₂CF₃ SO₂Me 11.98 (s, 1H), 8.14 (d, 1H), 7.99 (d, 1H), 6.10-6.00 (m, 1H), 5.34 (dd, 1H), 5.26 (s, 2H), 5.23 (dd, 1H), 5.06 (d, 2H), 4.30 (q, 2H), 3.39 (s, 3H) 7-28 N CH₂OMe Cl CH₂OCH₂CF₃ SO₂Me 7-29 CH nPr Me SO₂Me CF₃ 7-30 CH iPr Me SO₂Me CF₃ 7.80 (s, 2H), 7.78 (s, 1H), 4.77 (m, 1H), 3.22 (s, 3H), 2.82 (s, 3H), 1.48 (d, 6H) 7-31 CH pyrid-2-yl Me SO₂Me CF₃ 12.43 (brs), 8.37 (d, 1H),8.05 (d, 1H), 7.98- 7.82 (m, 4H), 7.31 (dd, 1H), 3.29 (s, 3H), 2.92 (s, 3H) 7-32 N nPr Me SO₂Me CF₃ 7.89 (m, 2H), 4.41 (t, 2H), 3.27 (s, 3H), 2.83 (s, 3H), 2.03 (m, 2H), 1.00 (t, 3H) 7-33 N iPr Me SO₂Me CF₃ 8.08 (d, 1H), 8.06 (d, 1H), 4.78 (m, 1H), 3.44 (s, 3H), 2.76 (s, 3H), 1.53 (d,6H) 7-34 N cPr Me SO₂Me CF₃ 7.80 (s, 2H), 3.75 (m, 3H), 3.23 (s, 3H), 2.76 (s, 3H), 1.28-1.18 (m, 4H) 7-35 N allyl Me SO₂Me CF₃ 7.88-7.78 (m, 2H), 6.02- 5.92 (m, 1H), 5.24-5.19 (m, 1H), 5.08-4.99 (m, 1H), 4.76-4.53 (m, 2H), 3.39 (s, 3H), 2.75 (s 3H) 7-36 N CH₂OMe Me SO₂Me CF₃ 11.89 (s, 1H), 8.09 (d, 1H), 7.97 (d, 1H), 5.60 (s, 2H), 3.41 (s, 3H), 2.69 (s, 3H), 2.22 (s, 3H) 7-37 N CH₂(CO)Me Me SO₂Me CF₃ 11.89 (s, 1H), 8.09 (d, 1H), 7.97 (d, 1H), 5.60 (s, 2H), 3.41 (s, 3H), 2.69 (s, 3H), 2.22 (s, 3H) 7-38 N CH₂COOEt Me SO₂Me CF₃ 12.02 (s, 1H), 8.06 (d, 1H), 8.02 (d, 1H), 5.49 (s, 2H), 4.20 (q, 2H), 3.43 (s, 3H), 2.71 (s, 3H), 1.12 (t, 3H) 7-39 N 4-Cl-benzyl Me SO₂Me CF₃ 11.87 (s, 1H), 8.05 (d,1 H), 7.96 (d, 1H), 7.48 (d, 2H), 7.32 (d, 2H), 5.67 (s, 2H), 3.42 (s, 3H), 2.67 (s, 3H) 7-40 CH nPr Me SO₂Me SO₂Me 7-41 CH iPr Me SO₂Me SO₂Me 7-42 N nPr Me SO₂Me SO₂Me 8.37 (d, 1H), 7.89 (d, 1H), 4.39 (t, 2H), 3.58 (s, 3H), 3.49 (s, 3H), 2.86 (s, 3H), 2.03 (m, 2H), 1.01 (t, 3H) 7-43 N iPr Me SO₂Me SO₂Me 7-44 N cPr Me SO₂Me SO₂Me 7-45 N CH₂OMe Me SO₂Me SO₂Me 7-46 N CH₂(CO)Me Me SO₂Me SO₂Me 11.89 (s, 1H), 8.26 (d, 1H), 8.05 (d, 1H), 5.59 (s, 2H), 3.57 (s, 3H), 3.40 (s, 3H), 2.66 (s, 3H), 2.25 (s, 3H) 7-47 N CH₂COOEt Me SO₂Me SO₂Me 12.03 (s, 1H), 8.27 (d, 1H), 8.06 (d, 1H), 5.47 (s, 2H), 4.20 (q, 2H), 3.60 (s, 3H), 3.41 (s, 3H), 2.63 (s, 3H), 1.12 (t, 3H) 7-48 N 4-Cl-benzyl Me SO₂Me SO₂Me 11.89 (s, 1H), 8.27 (d, 1H), 8.00 (d, 1H), 7.48 (d, 2H), 7.32 (d, 2H), 5.67 (s, 2H), 3.60 (s, 3H), 3.57 (s, 3H), 2.64 (s, 3H) 7-49 N allyl SMe H CF₃ 8.10 (d, 1H), 7.46 (d, 1H), 0 6,05-5.98 (m, 1H), 5.22 (d, 0 1H), 5.16-5.08 (m, 1H), 4.93 (d, 2H), 2.42 (s, 3H), 2.08 (s 3H) 7-50 N nBu SO₂Me H CF₃ 8.35 (d, 1H), 8.31 (s, 1H), 8.13 (d, 1H), 4.39 (t, 2H), 3.45 (s, 3H), 1.85 (m, 2H), 1.32 (m, 2H), 0.91 (t, 3H) 7-51 N nBu Me Cl SO₂Me 8.18 (d, 1H), 7.67 (d, 1H), 4.43 (t, 2H), 3.33 (s, 3H), 2.62 (s, 3H), 1.99 (m, 2H), 1.42 (m, 2H), 0.99 (t, 3H) 7-52 N allyl F SMe CF₃ 11.84 (s, 1H), 7.92 (t, 1H), 7.81 (d, 1H), 6.07-5.97 (m, 1H), 5.34 (d, 1H), 5.25 (d, 1H), 5.04 (d, 2H) 7-53 N allyl F SO₂Me CF₃ 11.98 (s, 1H), 8.28 (t, 1H), 8.05 (d, 1H), 6.07-5.97 (m, 1H), 5.33 (d, 1H), 5.26 (d, 1H), 5.04 (d, 2H), 3.51 (s, 3H) 7-54 N allyl Cl Me SMe 11.61 (s, 1H), 7.50 (d, 1H), 7.31 (d, 1H), 6,06-5.97 (m, 1H), 5.32 (d, 1H), 5.21 (d, 1H), 5.02 (d, 2H), 3.25 (s, 3H), 2.66 (s, 3H) 7-55 N allyl Cl 5-cyanomethyl- SO₂Et 11.80 (s, 1H), 7.98 (d, 1H), 4,5-dihydro-1,2- 7.88 (d, 1H), 6.04-5.94 (m, oxazol-3-yl 1H), 5.21 (d, 1H), 5.13 (d, 1H), 4.84 (d, 2H), 3.59 (m, 1H), 3.38 (q, 2H), 3.13 (dd, 1H), 3.06-2.95 (m, 4H), 1.15 (t, 3H) 7-56 N allyl Cl CH₂OCH₂- SO₂Me 11.96 (s, 1H), 8.12 (d, 1H), tetrahydrofuran- 7.95 (d, 1H), 6.08-6,00 (m, 2-yl 1H), 5.34 (d, 1H), 5.25 (d, 1H), 5.07 (s, 2H), 5.07 (d, 2H), 4.00-3.95 (m, 1H), 3.72 (q, 1H), 3.62-3.53 (m, 3H), 3.40 (s, 3H), 3.30 (s, 3H), 1.93-1.75 (m, 3H), 1.58-1.51 (m, 1H) 7-57 N allyl Me SO₂Me SO₂Me 11.83 (s, 1H), 8.28 (d, 1H), 8.09 (d, 1H), 6.11-5.97 (m, 1H), 5.34 (d, 1H), 5.21 (d, 1H), 5.06 (d, 2H), 3.61 (s, 3H), 3.58 (s, 3H), 2.71 (s 3H) 7-58 N nBu Me SO₂Me SO₂Me 8.37 (d, 1H), 7.92 (d, 1H), 4.44 (t, 2H), 3.58 (s, 3H), 3.50 (s, 3H), 2.86 (s, 3H), 1.98 (m, 2H), 1.41 (m, 2H), 0.99 (t, 3H) 7-59 N n-Pr Me SMe CN 7.72 (d, 1H), 7.71 (d, 1H), 4.42 (t, 2H), 2.75 (s, 3H), 2.52 (s, 3H), 2.02 (sex, 2H), 0.99 (t, 3H) 7-60 N n-Pr Me SOMe CN 7-61 N n-Pr Me SO₂Me CN 7-62 N allyl Me SOMe CF₃ 11.80 (s, 1H), 7.89 (2d, 2H), 6.10-6.00 (m, 1H), 5.34 (d, 1H), 5.22 (d, 1H), 5.07 (d, 2H), 3.06 (s, 3H), 2.87 (s 3H) 7-63 N 2-methyl- Me SMe CF₃ 7.62 (d, 1H), 7.54 (d, 1H), prop-1-yl 4.24 (d, 2H), 2.73 (s, 3H), 2.29 (s, 3H), 2.3-2.18 (m, 1H), 0.97 (d, 3H), 0.94 (d, 3H) 7-64 N 2-methyl- Me SO₂Me CF₃ 8.03 (d, 1H), 8.00 (d, 1H), prop-1-yl 4.18 (d, 2H), 3.42 (s, 3H), 2.76 (s, 3H), 2.25-2.15 (m, 1H), 0.88 (d,6H) 7-65 N 2,2-dimethyl- Me SO₂Me CF₃ 11.7 (brs, 1H), 8.07 (d, 1H), prop-1-yl 8.00 (d, 1H), 4.24 (s, 2H), 3.44 (s, 3H), 2.75 (s, 3H), 0.95 (s,9H) 7-66 N cyclopropyl- Me SMe CF₃ 7.77 (d, 1H), 7.73 (d, 1H), methyl 4.19 (d, 2H), 2.70 (s, 3H), 2.31 (s, 3H), 1.35 (m, 1H), 0.60-0.55 (m, 2H), 0.47-0.40 (m, 2H) 7-67 N cyclopropyl- Me SO₂Me CF₃ 7.95 (d, 1H), 7.90 (d, 1H), methyl 4.12 (d, 2H), 3.40 (s, 3H), 2.75 (s, 3H), 1.31 (m, 1H), 0.56-0.51 (m, 2H), 0.44-0.38 (m, 2H) 7-68 N CH₂(CO)Me CH₂SO₂Me H CF₃ 11.95 (s, 1H), 7.97 (2d, 2H), 5.54 (s, 2H), 4.97 (s, 2H), 3.03 (s, 3H), 2.21 (s, 3H) 7-69 N CH₂(CO)Me Me SMe CF₃ 11.76 (s, 1H), 7.80 (d, 1H), 7.70 (d, 1H), 5.58 (s, 2H), 2.64 (s, 3H), 2.31 (s, 3H), 2.07 (s, 3H) 7-70 N CH₂(CO)Me Me NMe₂ SO₂Me 7.85 (d, 1H), 7.56 (d, 1H), 5.56 (s, 2H), 2.82 (s, 3H), 2.24 (s, 3H) 7-71 N CH₂(CO)Me F SMe CF₃ 11.90 (s, 1H), 7.87 (t, 1H), 7.80 (d, 1H), 5.56 (s, 2H), 2.24 (s, 3H) 7-72 N CH₂(CO)Me Cl 5-cyanomethyl- SO₂Et 12.07 (s, 1H), 8.14 (d, 1H), 4,5-dihydro-1,2- 8.08 (d, 1H), 5.58 (s, 2H), oxazol-3-yl 5.18 (m, 1H), 3.64-3.57 (m, 1H), 3.42 (q, 2H), 3.15 (dd, 1H), 3.03-2.98 (m, 2H), 2.23 (s, 3H), 1.16 (t, 3H) 7-73 N CH₂(CO)Me Cl Cl SO₂Me 12.08 (s, 1H), 8.16 (d, 1H), 7.94 (d, 1H), 5.59 (s, 2H), 3.60 (s, 3H), 2.25 (s, 3H) 7-74 N CH₂COOEt F SMe CF₃ 12.04 (s, 1H), 7.89 (t, 1H), 7.81 (d, 1H), 546 (s, 2H), 4.19 (q, 2H), 1.21 (t, 3H) 7-75 N CH₂COOEt Cl CH₂-(4-methyl- Cl 7.65 (d, 1H), 7.59 (d, 1H), 1,2,4-triazolin- 7.46 (d, 2H), 7.31 (d, 2H), 5-on-1-yl) 5.63 (s, 2H), 5.05 (s, 2H), 3.40 (s, 3H) 7-76 N CH₂COOEt Cl H SO₂Me 12.14 (s, 1H), 8.16 (s, 1H), 8.06 (dd, 1H), 7.96 (d, 1H), 5.47 (s, 2H), 4.19 (q, 2H), 3.44 (s, 3H), 1.21 (t, 3H) 7-77 N CH₂COOEt Cl CH₂OCH₂CF₃ SO₂Me 12.17 (s, 1H), 8.14 (d, 1H), 7.98 (d, 1H), 5.48 (s, 2H), 5.66 (s, 2H), 5.25 (s, 2H), 4.29 (q, 2H), 4.19 (q, 2H), 3.36 (s, 3H), 1.21 (t, 3H) 7-78 N CH₂COOEt Cl Cl SO₂Me 12.20 (s, 1H), 8.17 (d, 1H), 7.95 (d, 1H), 5.48 (s, 2H), 4.20 (q, 2H), 3.48 (s, 3H), 1.21 (t, 3H) 7-79 N CH₂COOEt Cl CH₂OCH₂- SO₂Me 12.18 (s, 1H), 8.12 (d, 1H), tetrahydrofuran- 7.94 (d, 1H), 5.48 (s, 2H), 2-yl 5.08 (s, 2H), 4.19 (q, 2H), 4.00-3.95 (m, 1H), 3.75- 3.69 (q, 1H), 3.64-3.53 (m, 3H), 3.40 (s, 3H), 1.93- 1.76 (m, 3H), 1.58-1.51 (m, 1H), 1.21 (t, 3H) 7-80 N CH₂COOEt SO₂Me F CF₃ 12.24 (s, 1H), 8.33 (t, 1H), 8.17 (t, 1H), 7.81 (bs, 1H), 7.46 (d, 1H), 5.46 (s, 2H), 4.19 (q, 2H), 3.44 (s, 3H), 1.22 (t, 3H) 7-81 N tetrahydro- Me SO₂Me CF₃ 11.85 (brs, 1H), 8.07 (d, 1H), furan-2-yl- 8.00 (d, 1H), 4.59 (dd, 1H), methyl 4.45 (dd, 1H), 4.23 (m, 1H), 3.70-3.60 (m, 2H), 3.44 (s, 3H), 2.76 (s, 3H), 2.05- 1.99 (m, 1H), (m, 1H), 1.83- 1.61 (m, 3H), 7-82 N tetrahydro- Me SO₂Me CF₃ 7.97 (s, 2H), 5.17 (m, 1H), furan-3-yl 4.12-4.00 (m, 2H), 3.92-3.84 (m, 2H), 3.40 (s, 3H), 2.76 (s, 3H), 2.46-2.28 (m, 2H), (m, 1H), 1.83-1.61 (m, 3H), 7-83 N nBu Me SO₂Me CF₃ 8.06 (s, 2H), 4.35 (t, 2H), 3.44 (s, 3H), 2.76 (s, 3H), 1.85 (m, 2H), 1.31 (m, 2H), 0.91 (t, 3H) 7-84 N nHexyl Me SO₂Me CF₃ 7.93 (d, 2H), 7.88 (d, 2H), 4.20 (t, 2H), 3.39 (s, 3H), 2.75 (s, 3H), 1.79 (m, 1H), 1.68 (m, 1H), 1.30-1.20 (m,10H), 0.86 (m, 3H) 7-85 N propargyl Me SO₂Me CF₃ 7.97 (d, 1H), 7.85 (d, 1H), 4.96 (s 2H), 3.37 (s, 3H), 2.89 (s, 3H), 2.57 (t, 1H) 7-86 N CH₂CHF₂ Me SO₂Me CF₃ 7.84 (d, 1H), 7.77 (d, 1H), 6,43 (tt, 1H), 4.66 (m, 2H), 3.36 (s, 3H), 2.73 (s, 3H) 7-87 N CH₂CF₃ Me SO₂Me CF₃ 8.09 (d, 1H), 8.08 (d, 1H), 5.62 (q, 2H), 3.45 (s, 3H), 2.72 (s, 3H) 7-88 N CH₂OMe Me SO₂Me CF₃ 8.05 (d, 1H), 8.00 (d, 1H), 5.80 (s, 2H), 3.43 (s, 3H), 3.30 (s, 3H), 2.74 (s, 3H) 7-89 N CH₂CO(mor- Me SO₂Me CF₃ 8.05 (d, 1H), 7.97 (d, 1H), pholin-4-yl) 5.63 (s, 2H), 3.67-3.45 (m,8H), 3.44 (s, 3H), 2.68 (s, 3H) 7-90 N 2-methyl- Me SO₂Me CF₃ 7.94 (d, 1H), 7.85 (d, 1H), prop-2-en-1- 4.95 (s, 1H), 4.90 (s, 2H), yl 4.62 (s, 1H), 3.39 (s, 3H), 2.73 (s, 3H), 1.65 (s, 3H) 7-91 N 3-methylbut- Me SO₂Me CF₃ 7.97 (d, 1H), 7.89 (d, 1H), 2-en-1-yl 5.35 (t, 1H), 4.88 (d, 2H), 3.40 (s, 3H), 2.75 (s, 3H), 1.73 (s, 6H) 7-92 N 4-MeO- Me SO₂Me CF₃ 11.84 (brs, 1H), 8.05 (d, 1H), benzyl 7.92 (d, 1H), 7.24 (dd, 2H), 6.96 (dd, 2H), 5.58 (s, 2H), 3.75 (s, 3H), 3.43 (s, 3H), 2.68 (s, 3H) 7-93 N 4-Cl-benzyl Cl H SO₂Me 11.96 (s, 1H), 8.14 (s, 1H), 7.03 (dd, 1H), 7.89 (d, 1H), 7.48 (d, 2H), ), 7.32 (d, 2H), 5.65 (s, 2H) 7-94 N 4-Cl-benzyl Me NMe₂ SO₂Me 7.81 (d, 1H), 7.45-7.42 (m, 3H), 7.26 (d, 2H), 7.33 (d, 2H), 5.60 (s, 2H), 3.29 (s, 3H), 2.78 (s, 6H), 2.26 (s, 3H) 7-95 N 4-Cl-benzyl Me F SO₂Me 7.81 (t, 1H), 7.50-7.44 (m, 3H), 7.28 (d, 2H), 5.61 (s, 2H), 3.32 (s, 3H), 2.26 (s, 3H) 7-96 N 4-Cl-benzyl CF₃ F SO₂Me 12.15 (s, 1H), 8.31 (bs, 1H), 7.83 (bs, 1H), 7.49 (d, 2H), 7.33 (d, 2H), 5.63 (s, 2H), 3.49 (s, 3H) 7-97 N 4-Cl-benzyl F SMe CF₃ 7.97 (d, 1H), 7.93 (d, 1H), 7.59 (d, 2H), 7.44 (d, 2H), 5.76 (s, 2H), 3.61 (s, 3H) 7-98 N 4-Cl-benzyl Cl CH₂OCH₂CF₃ SO₂Me 12.03 (s, 1H), 8.13 (d, 1H), 7.92 (d, 1H), 7.49 (d, 2H), 7.33 (d, 2H), 5.66 (s, 2H), 5.24 (s, 2H), 4.28 (q, 2H), 3.37 (s, 3H) 7-99 N 4-Cl-benzyl Cl CH₂OCH₂- SO₂Me 12.04 (s, 1H), 8.11 (d, 1H), tetrahydrofuran- 7.88 (d, 1H), 7.49 (d, 2H), 2-yl 7.32 (d, 2H), 5.66 (s, 2H), 5.07 (dd, 2H), 3.99-3.94 (m, 1H), 3.73 (q, 2H), 3.69- 3.52 (m, 2H), 3.40 (s, 3H), 1.93-1.76 (m, 3H), 1.58- 1.51 (m, 1H) 7-100 N 4-Cl-benzyl Cl Cl SO₂Me 12.05 (s, 1H), 8.16 (d, 1H), 7.89 (d, 1H), 7.49 (d, 2H), 7.32 (d, 2H), 5.66 (s, 2H), 3.53 (s, 3H) 7-101 N 4-Cl-benzyl Cl SMe SO₂Me 11.98 (s, 1H), 8.14 (d, 1H), 7.87 (d, 1H), 7.49 (d, 2H), 7.33 (d, 2H), 5.66 (s, 2H), 3.63 (s, 3H) 7-102 N 4-Cl-benzyl SO₂Me F CF₃ 12.07 (s, 1H), 8.31 (t, 1H), 7.72 (bs, 1H), 7.48 (d, 2H), 7.38 (d, 2H), 5.65 (s, 2H), 3.55 (s, 3H) 7-103 N nPr Et H Br 8.95 (brs, 1H), 7.53 (s, 1H), 7.53 (s, 1H), 7.50 (s, 1H), 4.38 (t, 2H), 2.86 (q, 2H), 2.03 (m, 2H), 1.26 (t, 2H), 0.99 (t, 3H) 7-104 N nPr CF₃ H CF₃ 9.70 (brs, 1H), 8.08 (s, 1H), 7.98 (d, 1H), 7.91 (d, 1H), 4.38 (t, 2H), 2.03 (m, 2H), 1.00 (t, 3H) 7-105 N nPr Br H CF₃ 8.61 (brs, 1H), 7.98 (s, 1H), 7.83 (d, 1H), 7.77 (d, 1H), 4.40 (t, 2H), 2.06 (m, 2H), 1.01 (t, 3H) 7-106 N nPr SO₂Me H Cl 8.05 (d, 1H), 8.02 (d, 1H), 7.92 (d, 1H), 4.34 (t, 2H), 3.42 (s, 3H), 1.88 (m, 2H), 0.89 (t, 3H) 7-107 N nPr SO₂Me H Br 8.17 (s, 1H), 8.15 (d, 1H), 7.83 (d, 1H), 4.34 (t, 2H), 3.42 (s, 3H), 1.88 (m, 2H), 0.89 (t, 3H) 7-108 N nPr Me Cl CF₃ 7.37 (d, 1H), 7.27 (d, 1H), 4.19 (t, 2H), 2.33 (s, 3H), 1.84 (m, 2H), 0.90 (t, 3H) 7-109 N nPr Me SMe CF₃ 7.82 (d, 1H), 7.78 (d, 1H), 4.31 (t, 2H), 2.71 (s, 3H), 2.32 (s, 3H), 1.90 (m, 2H), 0.89 (t, 3H) 7-110 N n-Pr Me SEt CF₃ 7.74 (s, 2H), 4.42 (t, 2H), 2.81 (s, 3H), 2.78 (q, 2H), 2.04 (sex, 2H), 1.23 (t, 3H), 1.00 (t, 3H) 7-111 N n-Pr Me SO₂Et CF₃ 7.90 (d, 1H), 7.87 (d, 1H), 4.40 (t, 2H), 3.34 (q, 2H), 2.82 (s, 3H), 2.03 (sex, 2H), 1.48 (t, 3H), 1.00 (t, 3H) 7-112 N n-Pr Me SOEt CF₃ 7.77 (d, 1H), 7.69 (d, 1H), 4.38 (t, 2H), 3.42 (m, 1H), 2.92 (m, 1H), 2.87 (s, 3H), 2.02 (sex, 2H), 1.37 (t, 3H), 1.00 (t, 3H) 7-113 N n-Pr Me S(CH₂)₂OMe CF₃ 7-114 N n-Pr Me SO(CH₂)₂OMe CF₃ 7-115 N n-Pr Me SO₂(CH₂)₂OMe CF₃ 7-116 N n-Pr Me SMe NMe₂ 7-117 N n-Pr Me SOMe NMe₂ 7-118 N n-Pr Me SO₂Me NMe₂ 7-119 N n-Pr Me SMe imidazol- 1-yl 7-120 N n-Pr Me SO₂Me imidazol- 1-yl 7-121 N n-Pr Me SMe 1,2,4- triazol-1- yl 7-122 N n-Pr Me SOMe 1,2,4- triazol-1- yl 7-123 N n-Pr Me SO₂Me 1,2,4- triazol-1- yl 7-124 N nPr Me O(CH₂)₂OMe Cl 11.45 (brs, 1H), 7.50 (d, 1H), 7.41 (d, 1H), 4.28 (t, 2H), 4.05 (m, 2H), 3.68 (m, 2H), 3.34 (s, 3H), 2.37 (s, 3H), 1.88 (m, 2H), 0.88 (t, 3H) 7-125 N n-Pr Me SMe Cl 7.58 (d, 1H), 7.49 (d, 1H), 4.40 (t, 2H), 2.79 (s, 3H), 2.38 (s, 3H), 2.03 (sex, 2H), 0.99 (t, 3H) 7-126 N n-Pr Me SOMe Cl 7.73 (d, 1H), 7.57 (d, 1H), 4.30 (t, 2H), 3.04 (s, 3H), 2.72 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-127 N n-Pr Me SO₂Me Cl 7.86 (d, 1H), 7.75 (d, 1H), 4.30 (t, 2H), 3.46 (s, 3H), 2.72 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-128 N n-Pr Me SEt Cl 7.57 (d, 1H), 7.47 (d, 1H), 4.40 (t, 2H), 2.88 (q, 2H), 2.77 (s, 3H), 2.02 (sex, 2H), 1.22 (t, 3H), 0.99 (t, 3H) 7-129 N n-Pr Me SOEt Cl 7.73 (d, 1H), 7.59 (d, 1H), 4.30 (t, 2H), 3.40-3.24 (m, 1H), 3.19 (m, 1H), 2.71 (s, 3H), 1.89 (sex, 2H), 1.25 (t, 3H), 0.89 (t, 3H) 7-130 N n-Pr Me SO₂Et Cl 7.85 (d, 1H), 7.75 (d, 1H), 4.30 (t, 2H), 3.55 (q, 2H), 2.71 (s, 3H), 1.88 (sex, 2H), 1.23 (t, 3H), 0.89 (t, 3H) 7-131 N n-Pr Me S(CH₂)₂OMe Cl 7-132 N n-Pr Me SO(CH₂)₂OMe Cl 7-133 N n-Pr Me SO₂(CH₂)₂OMe Cl 7-134 N n-Pr Me SMe OMe 7-135 N n-Pr Me SOMe OMe 7-136 N n-Pr Me SO₂Me OMe 7-137 N n-Pr Me SEt OMe 7-138 N n-Pr Me SOEt OMe 7-139 N n-Pr Me SO₂Et OMe 7-140 N n-Pr Me SMe OEt 7.76 (d, 1H), 6.86 (d, 1H), 4.38 (t, 2H), 4.20 (q, 2H), 2.73 (s, 3H), 2.35 (s, 3H), 2.00 (sex, 2H), 1.53 (t, 3H), 0.97 (t, 3H) 7-141 N n-Pr Me SOMe OEt 7-142 N n-Pr Me SO₂Me OEt 7-143 N nPr Me 4,5-dihydro-1,2- SO₂Me 8.16 (d, 1H), 7.86 (d, 1H), oxazol-3-yl 4.62 (t, 2H), 4.40 (t, 2H), 3.31 (m, 2H), 3.25 (s, 3H), 2.49 (s, 3H), 2.06 (m, 2H), 1.00 (t, 3H) 7-144 N nPr Me F SMe 7.52 (d, 1H), 7.31 (t, 1H), 4.26 (t, 2H), 2.53 (s, 3H), 2.33 (d, 3H), 1.87 (m, 2H), 0.87 (t, 3H) 7-145 N nPr Me Cl SO₂Me 8.17 (d, 1H), 7.70 (d, 1H), 4.39 (t, 2H), 3.32 (s, 3H), 2.62 (s, 3H), 2.06 (m, 2H), 1.01 (t, 3H) 7-146 N nPr Me NH(CH₂)₂OEt SO₂Me 0.99 (t, 3H), 1.22 (t, 3H), 2.03 (m, 2H), 2.45 (s, 3H), 3.19 (s, 3H), 3.41 (m, 2H), 3.56 (q, 2H), 3.65 (m, 2H), 4.39 (t, 2H), 5.85 (s,br, 1H), 7.24 (d, 1H), 7.76 (d, 1H), 10.47 (s, 1H) 7-147 N nPr Me NHCH₂(1,3- SO₂Me dioxolan-2-yl) 7-148 N nPr Me pyrazol-1-yl SO₂Me 8.12 (d, 1H), 7.92 (d, 1H), 7.79 (d, 1H), 7.74 (d, 1H), 6.56 (dd, 1H), 4.35 (t, 2H), 2.87 (s, 3H), 2.03-1.95 (m, 5H), 0.98 (t, 3H) 7-149 N nPr Me O(CH₂)₂OMe SO₂Me 11.63 (brs, 1H), 7.83 (d, 1H), 7.62 (d, 1H), 4.30 (t, 2H), 4.16 (m, 2H), 3.76 (m, 2H), 3.38 (s, 3H), 3.37 (s, 3H), 2.41 (s, 3H), 1.89 (m, 2H), 0.89 (t, 3H) 7-150 N nPr Me tetrahydrofuran- SO₂Me 10.19 (bs, 1H), 7.97 (d, 1H), 2-ylmethoxy 7.63 (d, 1H), 4.39-4.43 (m, 3H), 4.07-4.10 (m, 2H), 3.96 (dd, 1H), 3.89 (dd, 1H), 3.32 (s, 3H), 2.55 (s, 3H), 2.06- 2.15 (m, 1H), 1.90-2.05 (m, 4H), 1.69-1.75 (m, 1H), 1.00 (t, 3H) 7-151 N n-Pr Me SEt SO₂Me 7-152 N n-Pr Me SOEt SO₂Me 7-153 N n-Pr Me SO₂Et SO₂Me 7-154 N nPr Me SMe SO₂Et 7-155 N nPr Me SOMe SO₂Et 7-156 N nPr Me SO₂Me SO₂Et 7-157 N nPr Me SEt SO₂Et 7-158 N nPr Me SOEt SO₂Et 7-159 N nPr Me SO₂Et SO₂Et 7-160 N n-Pr Me S(4-F-Ph) SO₂Me 7-161 N n-Pr Me SO(4-F-Ph) SO₂Me 7-162 N n-Pr Me SO₂(4-F-Ph) SO₂Me 7-163 N n-Pr Me SCH₂CF₃ SO₂Me 7-164 N n-Pr Me SOCH₂CF₃ SO₂Me 7-165 N n-Pr Me SO₂CH₂CF₃ SO₂Me 7-166 N n-Pr Me S(CH₂)₂OMe SO₂Me 7-167 N n-Pr Me SO(CH₂)₂OMe SO₂Me 7-168 N n-Pr Me SO₂(CH₂)₂OMe SO₂Me 7-169 N nPr Me S(CH₂)₂OMe SO₂Et 7-170 N n-Pr Me SO(CH₂)₂OMe SO₂Et 7-171 N n-Pr Me SO₂(CH₂)₂OMe SO₂Et 7-172 N nPr Et SMe CF₃ 0.99 (t, 3H), 1.26 (t, 3H), 2.03 (m, 2H), 2.34 (s, 3H), 3.22 (q, 2H), 4.41 (t, 2H), 7.53 (d, 1H), 7.63 (d, 1H), 10.78 (s, 1H) 7-173 N nPr Et SOMe CF₃ 1.00 (t, 3H), 1.25 (t, 3H), 2.03 (m, 2H), 3.03 (s, 3H), 3.42 (m, 1H), 3.62 (m, 1H), 4.41 (t, 2H), 7.72 (d, 1H), 7.79 (d, 1H), 10.85 (br,s, 1H) 7-174 N nPr Et SO₂Me CF₃ 1.00 (t, 3H), 1.36 (t, 3H), 2.05 (m, 2H), 3.31 (s, 3H), 3.36 (q, 2H), 4.42 (t, 2H), 7.88 (d, 1H), 7.92 (d, 1H), 9.60 (s, 1H) 7-175 N nPr Et SMe Cl 0.98 (t, 3H), 1.23 (t, 3H), 2.02 (m, 2H), 2.42 (s, 3H), 3.17 (q, 2H), 4.41 (t, 2H), 7.49 (d, 1H), 7.59 (d, 1H), 10.69 (s, 1H) 7-176 N nPr Et SOMe Cl 1.00 (t, 3H), 1.18 (t, 3H), 2.03 (m, 2H), 3.01 (m, 1H), 3.08 (s, 3H), 3.14 (m, 1H), 4.34 (t, 2H), 7.40 (d, 1H), 7.64 (d, 1H), 11.02 (s, 1H) 7-177 N nPr Et SO₂Me Cl 7-178 N nPr Et SMe Br 1.23 (t, 3H), 1.62 (t, 3H), 2.42 (s, 3H), 3.20 (q, 2H), 4.46 (q, 3H), 7.52 (d, 1H), 7.69 (d, 1H), 10.68 (s, 1H) 7-179 N nPr Et SOMe Br 1.00 (t, 3H), 1.18 (t, 3H), 2.02 (m, 2H), 3.06 (s, 3H), 3.11 (m, 1H), 3.17 (m, 1H), 4.37 (t, 2H), 7.53 (d, 1H), 7.62 (d, 1H), 11.02 (s, 1H) 7-180 N nPr Et SO₂Me Br 0.99 (t, 3H), 1.25 (t, 3H), 2.02 (m, 2H), 2.42 (s, 3H), 3.20 (q, 2H), 4.40 (t, 2H), 7.49 (d, 1H), 7.68 (d, 1H), 10.61 (s, 1H) 7-181 N n-Pr Et SEt CF₃ 7-182 N n-Pr Et SOEt CF₃ 7-183 N n-Pr Et SO₂Et CF₃ 7-184 N n-Pr Et S(CH₂)₂OMe CF₃ 7-185 N n-Pr Et SO(CH₂)₂OMe CF₃ 7-186 N n-Pr Et SO₂(CH₂)₂OMe CF₃ 7-187 N n-Pr Et SEt Cl 7-188 N n-Pr Et SOEt Cl 7-189 N n-Pr Et SO₂Et Cl 7-190 N n-Pr Et S(CH₂)₂OMe Cl 7-191 N n-Pr Et SO(CH₂)₂OMe Cl 7-192 N n-Pr Et SO₂(CH₂)₂OMe Cl 7-193 N nPr Et SMe SO₂Me 7-194 N nPr Et SOMe SO₂Me 7-195 N nPr Et SO₂Me SO₂Me 7-196 N n-Pr Et SMe SO₂Et 7-197 N n-Pr Et SOMe SO₂Et 7-198 N n-Pr Et SO₂Me SO₂Et 7-199 N n-Pr Et SEt SO₂Me 7-200 N n-Pr Et SOEt SO₂Me 7-201 N n-Pr Et SO₂Et SO₂Me 7-202 N n-Pr Et SEt SO₂Et 7-203 N n-Pr Et SOEt SO₂Et 7-204 N n-Pr Et SO₂Et SO₂Et 7-205 N n-Pr Et S(CH₂)₂OMe SO₂Me 7-206 N n-Pr Et SO(CH₂)₂OMe SO₂Me 7-207 N n-Pr Et SO₂(CH₂)₂OMe SO₂Me 7-208 N n-Pr Et S(CH₂)₂OMe SO₂Et 7-209 N n-Pr Et SO(CH₂)₂OMe SO₂Et 7-210 N n-Pr Et SO₂(CH₂)₂OMe SO₂Et 7-211 N nPr nPr SMe Cl 0.99 (m,6H), 1.60 (m, 2H), 2.01 (m, 2H), 2.41 (s, 3H), 3.13 (m, 2H), 4.40 (t, 2H), 7.48 (d, 1H), 7.59 (d, 1H), 10.67 (s, 1H) 7-212 N nPr nPr SOMe Cl 0.98 (t, 3H), 1.01 (t, 3H), 1.43 (m, 1H), 1.68 (m, 1H), 2.02 (m, 2H), 2.91 (m, 1H), 3.09 (s, 3H), 3.25 (m, 1H), 4.37 (t, 2H), 7.40 (d, 1H), 7.63 (d, 1H), 10.65 (s, 1H) 7-213 N nPr nPr SO₂Me Cl 0.94 (t, 3H), 0.99 (t, 3H), 1.68 (m, 2H), 2.02 (m, 2H), 3.24 (m, 2H), 3.38 (s, 3H), 4.42 (t, 2H), 7.52 (d, 1H), 7.65 (d, 1H), 10.68 (s, 1H) 7-214 N nPr nPr SMe Br 0.99 (m,6H), 1.62 (m, 2H), 2.01 (m, 2H), 2.41 (s, 3H), 3.15 (m, 2H), 4.40 (t, 2H), 7.49 (d, 1H), 7.68 (d, 1H), 10.58 (s, 1H) 7-215 N nPr nPr SOMe Br 0.98 (t, 3H), 1.02 (t, 3H), 1.50 (m, 1H), 1.68 (m, 1H), 2.03 (m, 2H), 3.05 (s, 3H), 3.16 (m, 1H), 3.25 (m, 1H), 4.47 (t, 2H), 7.52 (d, 1H), 7.62 (d, 1H), 10.56 (s, 1H) 7-216 N nPr nPr SO₂Me Br 0.94 (t, 3H), 0.99 (t, 3H), 1.68 (m, 2H), 2.03 (m, 2H), 3.25 (m, 2H), 3.37 (s, 3H), 4.43 (t, 2H), 7.52 (d, 1H), 7.80 (d, 1H), 10.68 (s, 1H) 7-217 N nPr nPr SMe CF₃ 0.99 (m,6H), 1.62 (m, 2H), 2.02 (m, 2H), 2.35 (s, 3H), 3.20 (m, 2H), 4.42 (t, 2H), 7.74 (s, 2H), 10.87 (s, 1H) 7-218 N nPr nPr SOMe CF₃ 7-219 N nPr nPr SO₂Me CF₃ 0.98 (t, 3H), 0.99 (t, 3H), 1.67 (m, 2H), 2.02 (m, 2H), 3.25 (m, 2H), 3.30 (s, 3H), 4.47 (t, 2H), 7.91 (s, 2H), 10.58 (s, 1H) 7-220 N nPr nPr SMe SO₂Me 7-221 N nPr nPr SOMe SO₂Me 7-222 N nPr nPr SO₂Me SO₂Me 7-223 N nPr iPr SMe Cl 0.99 (t, 3H), 1.43 (d,6H), 2.01 (m, 2H), 2.41 (s, 3H), 3.88 (br,s, 1H), 4.42 (t, 2H), 7.40 (d, 1H), 7.46 (d, 1H), 10.41 (s, 1H) 7-224 N nPr iPr SOMe Cl 7-225 N nPr iPr SO₂Me Cl 7-226 N nPr iPr SMe Br 7-227 N nPr iPr SOMe Br 7-228 N nPr iPr SO₂Me Br 7-229 N nPr iPr SMe CF₃ 7-230 N nPr iPr SOMe CF₃ 7-231 N nPr iPr SO₂Me CF₃ 7-232 N nPr iPr SMe SO₂Me 7-233 N nPr iPr SOMe SO₂Me 7-234 N nPr iPr SO₂Me SO₂Me 7-235 N nPr cPr SMe Cl 7-236 N nPr cPr SOMe Cl 7-237 N nPr cPr SO₂Me Cl 7-238 N nPr cPr SMe Br 7-239 N nPr cPr SOMe Br 7-240 N nPr cPr SO₂Me Br 7-241 N nPr cPr SMe CF₃ 7-242 N nPr cPr SOMe CF₃ 7-243 N nPr cPr SO₂Me CF₃ 7-244 N nPr cPr SMe SO₂Me 7-245 N nPr cPr SOMe SO₂Me 7-246 N nPr cPr SO₂Me SO₂Me 7-247 N n-Pr CH₂OMe F CF₃ 7-248 N n-Pr CH₂OMe SMe CF₃ 7-249 N n-Pr CH₂OMe SOMe CF₃ 7-250 N n-Pr CH₂OMe SO₂Me CF₃ 7-251 N n-Pr CH₂OMe SEt CF₃ 7-252 N n-Pr CH₂OMe SOEt CF₃ 7-253 N n-Pr CH₂OMe SO₂Et CF₃ 7-254 N n-Pr CH₂OMe S(CH₂)₂OMe CF₃ 7-255 N n-Pr CH₂OMe SO(CH₂)₂OMe CF₃ 7-256 N n-Pr CH₂OMe SO₂(CH₂)₂OMe CF₃ 7-257 N n-Pr CH₂OMe SMe Cl 7-258 N n-Pr CH₂OMe SOMe Cl 7-259 N n-Pr CH₂OMe SO₂Me Cl 7-260 N n-Pr CH₂OMe SEt Cl 7-261 N n-Pr CH₂OMe SOEt Cl 7-262 N n-Pr CH₂OMe SO₂Et Cl 7-263 N n-Pr CH₂OMe S(CH₂)₂OMe Cl 7-264 N n-Pr CH₂OMe SO(CH₂)₂OMe Cl 7-265 N n-Pr CH₂OMe SO₂(CH₂)₂OMe Cl 7-266 N n-Pr CH₂OMe Cl SO₂Me 8.31 (d, 1H), 7.87 (d, 1H), 4.91 (s, 2H), 4.38 (t, 2H), 3.60 (s, 3H), 3.33 (s, 3H), 2.03 (sex, 2H), 1.00 (t, 3H) 7-267 N n-Pr CH₂OMe SMe SO₂Me 7-268 N n-Pr CH₂OMe SOMe SO₂Me 7-269 N n-Pr CH₂OMe SO₂Me SO₂Me 7-270 N n-Pr CH₂OMe SMe SO₂Et 7-271 N n-Pr CH₂OMe SOMe SO₂Et 7-272 N n-Pr CH₂OMe SO₂Me SO₂Et 7-273 N n-Pr CH₂OMe SEt SO₂Me 7-274 N n-Pr CH₂OMe SOEt SO₂Me 7-275 N n-Pr CH₂OMe SO₂Et SO₂Me 7-276 N n-Pr CH₂OMe SEt SO₂Et 7-277 N n-Pr CH₂OMe SOEt SO₂Et 7-278 N n-Pr CH₂OMe SO₂Et SO₂Et 7-279 N n-Pr CH₂OMe S(CH₂)₂OMe SO₂Me 7-280 N n-Pr CH₂OMe SO(CH₂)₂OMe SO₂Me 7-281 N n-Pr CH₂OMe SO₂(CH₂)₂OMe SO₂Me 7-282 N n-Pr CH₂OMe S(CH₂)₂OMe SO₂Et 7-283 N n-Pr CH₂OMe SO(CH₂)₂OMe SO₂Et 7-284 N n-Pr CH₂OMe SO₂(CH₂)₂OMe SO₂Et 7-285 N n-Pr F SCH₂Ph CF₃ 7-286 N n-Pr F SMe F 7-287 N n-Pr F SOMe F 7-288 N n-Pr F SO₂Me F 7-289 N n-Pr F SEt Cl 7.97 (t, 1H), 7.46 (d, 1H), 4.32 (t, 2H), 3.01 (q, 2H), 2.01 (sex, 2H), 1.27 (t, 3H), 0.97 (t, 3H) 7-290 N n-Pr Cl SMe H 7-291 N n-Pr Cl SOMe H 7-292 N n-Pr Cl SO₂Me H 7-293 N n-Pr Cl SCF₂CF₂H H 7-294 N n-Pr Cl SOCF₂CF₂H H 7-295 N n-Pr Cl SO₂CF₂CF₂H H 7-296 N nPr Cl Me Cl 7.63 (d, 1H), 7.57 (d, 1H), 4.31 (q, 2H), 2.51 (s, 3H), 1.88 (m, 2H), 0.86 (t, 3H) 7-297 N nPr Cl Cl Cl 7.49 (d, 1H), 7.46 (d, 1H), 4.36 (q, 2H), 1.99 (m, 2H), 0.97 (t, 3H) 7-298 N n-Pr Cl SMe Cl 7.60 (d, 1H), 7.54 (d, 1H), 4.41 (t, 2H), 2.48 (s, 3H), 2.04 (sex, 2H), 0.99 (t, 3H) 7-299 N n-Pr Cl SOMe Cl 7.70 (d, 1H), 7.52 (d, 1H), 4.39 (t, 2H), 3.11 (s, 3H), 2.03 (sex, 2H), 0.99 (t, 3H) 7-300 N n-Pr Cl SO₂Me Cl 7.71 (d, 1H), 7.65 (d, 1H), 4.43 (t, 2H), 3.42 (s, 3H), 2.03 (sex, 2H), 0.99 (t, 3H) 7-301 N n-Pr Cl SEt Cl 7-302 N n-Pr Cl SOEt Cl 7-303 N n-Pr Cl SO₂Et Cl 7-304 N n-Pr Cl S(CH₂)₂OMe Cl 7-305 N n-Pr Cl SO(CH₂)₂OMe Cl 7-306 N n-Pr Cl SO₂(CH₂)₂OMe Cl 7-307 N nPr Cl CH₂OMe SO₂Me 1.00 (t, 3H), 2.02 (m, 2H), 3.27 (s, 3H), 3.52 (s, 3H), 4.44 (t, 2H), 5.10 (s, 2H), 7.77 (d, 1H), 8.16 (d, 1H), 10.75 (s, 1H) 7-308 N nPr Cl CH₂OEt SO₂Me 1.00 (t, 3H), 1.25 (t, 3H), 2.02 (m, 2H), 3.30 (s, 3H), 3.71 (q, 2H), 4.43 (t, 2H), 5.14 (s, 2H), 7.77 (d, 1H), 8.15 (d, 1H), 10.6 (s, 1H) 7-309 N nPr Cl CH₂OCH₂iPr SO₂Me 0.92 (d,6H), 1.00 (t, 3H), 1.90 (m, 1H), 2.04 (m, 2H), 3.28 (s, 3H), 3.43 (d, 2H), 4.43 (t, 2H), 5.11 (s, 2H), 7.77 (d, 1H), 8.15 (d, 1H), 10.49 (s, 1H) 7-310 N nPr Cl CH₂OCH₂cPr SO₂Me 0.25 (m, 2H), 0.25 (m, 2H), 1.00 (t, 3H), 1.11 (m, 1H), 2.04 (m, 2H), 3.33 (s, 3H), 3.49 (d, 2H), 4.43 (t, 2H), 5.16 (s, 2H), 7.78 (d, 1H), 8.16 (d, 1H), 10.6 (s, 1H) 7-311 N nPr Cl CH₂OC₂H₄OMe SO₂Me 0.99 (t, 3H), 2.03 (m, 1H), 3.32 (s, 3H), 3.35 (s, 3H), 3.58 (m, 2H), 3.79 (m, 2H), 4.42 (t, 2H), 5.19 (s, 2H), 7.78 (d, 1H), 8.12 (d, 1H), 10.89 (s, 1H) 7-312 N nPr Cl CH₂OC₂H₄OEt SO₂Me 1.00 (t, 3H), 1.16 (t, 3H), 2.03 (m, 1H), 3.35 (s, 3H), 3.48 (q, 2H), 3.62 (m, 2H), 3.80 (m, 2H), 4.42 (t, 2H), 5.21 (s, 2H), 7.77 (d, 1H), 8.15 (d, 1H), 10.32 (s, 1H) 7-313 N nPr Cl CH₂(2- SO₂Me 0.98 (t, 3H), 1.98 (m,4H), oxopyrrolidin-1- 2.35 (m, 2H), 3.21 (s, 3H), yl) 3.28 (m, 2H), 4.40 (t, 2H), 5.02 (s, 2H), 7.73 (d, 1H), 8.16 (d, 1H) 7-314 N n-Pr Cl F SMe 7.66 (d, 1H), 7.31-7.13 (m, 1H), 4.37 (t, 2H), 2.54 (s, 3H), 2.03 (m, 2H), 0.98 (t, 3H) 7-315 N n-Pr Cl F SOMe 7.86 (dd, 1H), 7.76 (d, 1H), 4.43 (t, 2H), 2.92 (s, 3H), 2.04 (q, 2H), 1.00 (t, 3H) 7-316 N n-Pr Cl F SO₂Me 8.02 (t, 1H), 7.72 (d, 1H), 4.41 (t, 2H), 3.30 (s, 3H), 2.04 (q, 2H), 1.00 (t, 3H) 7-317 N nPr Cl OMe SO₂Me 10.00 (bs, 1H), 8.03 (d, 1H), 7.62 (d, 1H), 4.43 (t, 2H), 4.14 (s, 3H), 3.29 (s, 3H), 2.04 (sex, 2H), 1.00 (t, 3H) 7-318 N nPr Cl OMe SO₂Et 11.90 (s, 1H), 7.92 (d, 1H), 7.76 (d, 1H), 4.32 (t, 2H), 4.01 (s, 3H), 3.50 (q, 2H), 1.89 (quin, 2H), 1.12 (t, 3H), 0.88 (t, 3H) 7-319 N nPr Cl OEt SO₂Et 11.90 (s, 1H), 7.93 (d, 1H), 7.74 (d, 1H), 4.32 (t, 2H), 4.22 (q, 2H), 3.52 (q, 2H), 1.89 (quin, 2H), 1.45 (t, 3H), 1.12 (t, 3H), 0.88 (t, 3H) 7-320 N nPr Cl OEt SO₂Me 10.02 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.43 (t, 2H), 4.35 (q, 2H), 3.30 (s, 3H), 2.04 (sex, 2H), 1.54 (t, 3H), 1.00 (t, 3H) 7-321 N nPr Cl OPr SO₂Et 11.84 (bs, 1H), 7.93 (d, 1H), 7.74 (d, 1H), 4.32 (t, 2H), 4.15 (t, 2H), 3.50 (q, 2H), 1.88 (sep, 4H), 1.13 (t, 3H), 1.05 (t, 3H), 0.89 (t, 3H) 7-322 N nPr Cl OPr SO₂Me 10.55 (bs, 1H), 8.02 (d, 1H), 7.58 (d, 1H), 4.44 (t, 2H), 4.25 (t, 2H), 3.30 (s, 3H), 2.04 (quin, 2H), 1.96 (quin, 2H), 1.10 (t, 3H), 1.00 (t, 3H) 7-323 N nPr Cl OiPr SO₂Et 11.93 (s, 1H), 7.95 (d, 1H), 7.70 (d, 1H), 4.15-4.25 (m, 1H), 4.32 (t, 2H), 3.48 (q, 2H), 1.88 (quin, 2H), 1.34 (d, 6H), 1.09 (t, 3H), 0.88 (t, 3H) 7-324 N nPr Cl allyloxy SO₂Et 11.90 (bs, 1H), 7.95 (d, 1H), 7.79 (d, 1H), 6.19 (m, 1H), 5.51 (d, 1H), 5.35 (d, 1H), 4.69-4.72 (m, 2H), 4.32 (q, 2H), 3.51 (q, 2H), 1.89 (sex, 2H), 1.12 (t, 3H), 0.88 (t, 3H) 7-325 N nPr Cl allyloxy SO₂Me 11.91 (bs, 1H), 7.97 (d, 1H), 7.78 (d, 1H), 6.20 (m, 1H), 5.51 (d, 1H), 5.37 (d, 1H), 4.70-4.73 (m, 2H), 4.32 (t, 2H), 3.39 (s, 3H), 1.89 (sex, 2H), 0.88 (t, 3H) 7-326 N nPr Cl propargyloxy SO₂Et 10.10 (bs, 1H), 8.02 (d, 1H), 7.65 (d, 1H), 4.97 (d, 2H), 4.43 (t, 2H), 3.51 (q, 2H), 2.67 (t, 1H), 2.04 (quin, 2H), 1.29 (t, 3H), 1.00 (t, 3H) 7-327 N nPr Cl propargyloxy SO₂Me 10 95 (bs, 1H), 8.03 (d, 1H), 7.64 (d, 1H), 4.99 (d, 2H), 4.44 (t, 2H), 3.34 (s, 3H), 2.68 (t, 1H), 2.03 (quin, 2H), 1.00 (t, 3H) 7-328 N nPr Cl OCH₂CH₂F SO₂Me 11.10 (bs, 1H), 8.05 (d, 1H), 7.64 (d, 1H), 4.91 (bs, 1H), 4.83 (bs, 1H), 4.61 (bs, 1H), 4.56 (bs, 1H), 4.45 (t, 2H), 3.34 (s, 3H), 2.04 (quin, 2H), 0.99 (t, 3H) 7-329 N nPr Cl OCH₂CH₂F SO₂Et 10.90 (bs, 1H), 8.04 (d, 1H), 7.64 (d, 1H), 4.90 (bs, 1H), 4.82 (bs, 1H), 4.60 (bs, 1H), 4.55 (bs, 1H), 4.45 (t, 2H), 3.51 (q, 2H), 2.03 (quin, 2H), 1.29 (t, 3H), 0.99 (t, 3H) 7-330 N nPr Cl OCH₂CN SO₂Et 11.60 (bs, 1H), 8.02 (d, 1H), 7.70 (d, 1H), 5.09 (s, 2H), 4.46 (t, 2H), 3.45 (q, 2H), 2.01 (quin, 2H), 1.32 (t, 3H), 1.00 (t, 3H) 7-331 N nPr Cl OCH₂(CO)NMe₂ SO₂Et 11.91 (s, 1H), 7.94 (d, 1H), 7.71 (d, 1H), 4.89 (s, 2H), 4.32 (t, 2H), 3.71 (q, 2H), 2.89 (s, 3H), 2.99 (s, 3H), 1.89 (quin, 2H), 1.11 (t, 3H), 0.89 (t, 3H) 7-332 N nPr Cl O(CH₂)₂OMe SO₂Me 11.86 (brs, 1H), 7.96 (d, 1H), 7.74 (d, 1H), 4.32 (t, 2H), 4.32 (m, 2H), 3.76 (m, 2H), 3.40 (s, 3H), 3.37 (s, 3H), 1.89 (m, 2H), 0.89 (t, 3H) 7-333 N nPr Cl O(CH₂)₂OMe SO₂Et 11.90 (s, 1H), 7.93 (d, 1H), 7.77 (d, 1H), 4.33 (t, 2H), 4.32 (t, 2H), 3.78 (t, 2H), 3.57 (q, 2H), 1.89 (quin, 2H), 1.13 (t, 3H), 0.88 (t, 3H) 7-334 N nPr Cl O(CH₂)₃OMe SO₂Me 9.90 (bs, 1H), 8.03 (d, 1H), 7.61 (d, 1H), 4.42 (t, 2H), 4.38 (t, 2H), 3.63 (t, 2H), 3.38 (s, 3H), 3.29 (s, 3H), 2.21 (quin, 2H), 2.04 (sex, 2H), 1.00 (t, 3H) 7-335 N nPr Cl O(CH₂)₃OMe SO₂Et 7.93 (d, 1H), 7.74 (d, 1H), 4.34 (t, 2H), 4.23 (m, 2H), 3.58-3.51 (m,4H), 3.27(s, 3H), 2.09 (m, 2H), 1.88 (m, 2H), 1.12 (t, 3H), 0.89 (t, 3H) 7-336 N nPr Cl O(CH₂)₂OEt SO₂Me 10.21 (bs, 1H), 8.04 (d, 1H), 7.61 (d, 1H), 4.47 (t, 2H), 4.42 (t, 2H), 3.90-3.92 (m, 2H), 3.64 (q, 2H), 3.35 (s, 3H), 2.04 (sex, 2H), 1.26 (t, 3H), 1.00 (t, 3H) 7-337 N nPr Cl O(CH₂)₂OEt SO₂Et 10.10 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.46 (t, 2H), 4.43 (t, 2H), 3.89-3.91 (m, 2H), 3.63 (q, 2H), 3.52 (q, 2H), 2.03 (sex, 2H), 1.27 (t, 3H), 1.26 (t, 3H), 1.00 (t, 3H) 7-338 N nPr Cl O(CH₂)₂OCF₃ SO₂Et 10.76 (bs, 1H), 8.03 (d, 1H), 7.64 (d, 1H), 4.54-4.56 (m, 2H), 4.41-4.46 (m, 4H), 3.47 (q, 2H), 2.03 (sex, 2H), 1.30 (t, 3H), 1.00 (t, 3H) 7-339 N nPr Cl O(CH₂)₃OCF₃ SO₂Et 10.70 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.39-4.46 (m, 4H), 4.26 (t, 2H), 3.41 (q, 2H), 2.31 (quin, 2H), 2.03 (sex, 2H), 1.29 (t, 3H), 1.00 (t, 3H) 7-340 N nPr Cl O(CH₂)₃OCF₃ SO₂Me 10.33 (bs, 1H), 8.04 (d, 1H), 7.62 (d, 1H), 4.40-4.45 (m, 4H), 4.26 (t, 2H), 3.26 (s, 3H), 2.33 (quin, 2H), 2.04 (sex, 2H), 1.00 (t, 3H) 7-341 N nPr Cl O(CH₂)₂OCF₃ SO₂Me 10.75 (bs, 1H), 8.03 (d, 1H), 7.64 (d, 1H), 4.57 (t, 2H), 4.42-4.46 (m, 4H), 3.31 (s, 3H), 2.03 (sex, 2H), 1.00 (t, 3H) 7-342 N nPr Cl O(CH₂)₂SMe SO₂Et 10.29 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.43 (t, 2H), 3.51 (q, 2H), 3.02 (t, 2H), 2.22 (s, 3H), 2.03 (quin, 2H), 1.28 (t, 3H), 1.00 (t, 3H) 7-343 N nPr Cl O(CH₂)₂SMe SO₂Me 10.40 (bs, 1H), 8.04 (d, 1H), 7.62 (d, 1H), 4.45 (t, 2H), 4.43 (t, 2H), 3.34 (s, 3H), 3.03 (t, 2H), 2.22 (s, 3H), 2.04 (sex, 2H), 1.00 (t, 3H) 7-344 N nPr Cl O(CH₂)₃SMe SO₂Me 10.32 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.43 (t, 2H), 4.39 (t, 2H), 3.29 (s, 3H), 2.75 (t, 2H), 2.23 (t, 2H), 2.16 (s, 3H), 2.04 (sex, 2H), 1.00 (t, 3H) 7-345 N nPr Cl O(CH₂)₃SMe SO₂Et 10.62 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.44 (bt, 2H), 4.37 (bt, 2H), 3.45 (q, 2H), 2.75 (bt, 2H), 2.20-2.23 (m, 2H), 2.16 (s, 3H), 2.01-2.05 (m, 2H), 1.28 (t, 3H), 1.00 (t, 3H) 7-346 N nPr Cl O(CH₂)₂SEt SO₂Me 10.30 (bs, 1H), 8.04 (d, 1H), 7.62 (d, 1H), 4.43 (t, 2H), 3.34 (s, 3H), 3.07 (t, 2H), 2.66 (q, 2H), 2.04 (sex, 2H), 1.31 (t, 3H), 1.00 (t, 3H) 7-347 N nPr Cl O(CH₂)₂SEt SO₂Et 10.38 (bs, 1H), 8.02 (d, 1H), 7.61 (d, 1H), 4.40-4.50 (m, 4H), 3.51 (q, 2H), 3.05 (t, 2H), 3.64 (q, 2H), 2.04 (sex, 2H), 1.31 (t, 3H), 1.28 (t, 3H), 1.00 (t, 3H) 7-348 N nPr Cl OCH₂(CO)NMe₂ SO₂Me 7.94 (d, 1H), 7.72 (d, 1H), 4.87 (s, 2H), 4.29 (t, 2H), 3.46 (s, 3H), 2.88 (s, 3H), 2.86 (s, 3H), 1.85 (quin, 2H), 0.84 (t, 3H) 7-349 N nPr Cl 1,4-dioxan-2- SO₂Et 10.70 (bs, 1H), 8.02 (d, 1H), ylmethoxy 7.61 (d, 1H), 4.44 (t, 2H), 4.38 (dd, 1H), 4.21 (dd, 1H), 4.10-4.17 (m, 1H), 3.65- 3.96 (m, 5H), 3.58 (dd, 1H), 3.48 (q, 2H), 2.02 (quin, 2H), 1.28 (t, 3H), 0.99 (t, 3H) 7-350 N n-Pr Cl SMe SO₂Me 7-351 N n-Pr Cl SOMe SO₂Me 7-352 N n-Pr Cl SO₂Me SO₂Me 7-353 N n-Pr Cl SEt SO₂Me 7-354 N n-Pr Cl SOEt SO₂Me 7-355 N n-Pr Cl SO₂Et SO₂Me 7-356 N n-Pr Cl S(CH₂)₂OMe SO₂Me 7-357 N n-Pr Cl SO(CH₂)₂OMe SO₂Me 7-358 N n-Pr Cl SO₂(CH₂)₂OMe SO₂Me 7-359 N n-Pr OH SMe CHF₂ 7-360 N n-Pr OH SO₂Me CHF₂ 7-361 N n-Pr OH SOMe CHF₂ 7-362 N n-Pr OH SCH₂Ph CF₃ 7-363 N n-Pr OMe SMe CHF₂ 7-364 N n-Pr OMe SO₂Me CHF₂ 7-365 N n-Pr OMe SOMe CHF₂ 7-366 N n-Pr OMe SEt CF₃ 7-367 N n-Pr OMe SOEt CF₃ 7-368 N n-Pr OMe SO₂Et CF₃ 7-369 N n-Pr OMe S(CH₂)₂OMe CF₃ 7-370 N n-Pr OMe SO(CH₂)₂OMe CF₃ 7-371 N n-Pr OMe SO₂(CH₂)₂Me CF₃ 7-372 N n-Pr OMe SMe F 7-373 N n-Pr OMe SOMe F 7-374 N n-Pr OMe SO₂Me F 7-375 N n-Pr OMe SMe Cl 7-376 N n-Pr OMe SOMe Cl 7-377 N n-Pr OMe SO₂Me Cl 7-378 N n-Pr OMe SEt Cl 7-379 N n-Pr OMe SOEt Cl 7-380 N n-Pr OMe SO₂Et Cl 7-381 N n-Pr OMe S(CH₂)₂OMe Cl 7-382 N n-Pr OMe SO(CH₂)₂OMe Cl 7-383 N n-Pr OMe SO₂(CH₂)₂OMe Cl 7-384 N n-Pr OMe SMe OMe 7-385 N n-Pr OMe SOMe OMe 7-386 N n-Pr OMe SO₂Me OMe 7-387 N n-Pr OEt SMe CF₃ 7-388 N n-Pr OEt SOMe CF₃ 7-389 N n-Pr OEt SO₂Me CF₃ 7-390 N n-Pr OEt SEt CF₃ 7-391 N n-Pr OEt SOEt CF₃ 7-392 N n-Pr OEt SO₂Et CF₃ 7-393 N n-Pr OEt S(CH₂)₂OMe CF₃ 7-394 N n-Pr OEt SO(CH₂)₂OMe CF₃ 7-395 N n-Pr OEt SO₂(CH₂)₂OMe CF₃ 7-396 N n-Pr OEt SMe Cl 7-397 N n-Pr OEt SOMe Cl 7-398 N n-Pr OEt SO₂Me Cl 7-399 N n-Pr OEt SEt Cl 7-400 N n-Pr OEt SOEt Cl 7-401 N n-Pr OEt SO₂Et Cl 7-402 N n-Pr OEt S(CH₂)₂OMe Cl 7-403 N n-Pr OEt SO(CH₂)₂OMe Cl 7-404 N n-Pr OEt SO₂(CH₂)₂Me Cl 7-405 N n-Pr SO₂Me NMe₂ Cl 7-406 N n-Pr SO₂Me NHMe Cl 7-407 N n-Pr SO₂Me NH₂ Cl 7-408 N n-Pr SO₂Me NHc-Hex Cl 7-409 N n-Pr SO₂Me NMe₂ CF₃ 7-410 N n-Pr SO₂Me NHMe CF₃ 7-411 N nPr Me SOMe CF₃ 7.78 (s, 2H), 4.20 (t, 2H), 3.06 (s, 3H), 2.88 (s, 3H), 1.83 (m, 2H), 0.88 (t, 3H) 7-412 N nPr Cl 5- SO₂Et 0.99 (t, 3H), 1.28 (t, 3H), 2.02 methoxymethyl- (m, 2H), 3.28 (dd, 1H), 3.41 4,5-dihydro-1,2- (q, 2H), 3.46 (s, 3H), 3.51 oxazol-3-yl (dd, 1H), 3.60 (dd, 1H), 3.71 (dd, 1H), 4.42 (t, 2H), 5.06 (m, 1H), 7.92 (d, 1H), 8.14 (d, 1H), 11.1 (br, s, 1H) 7-413 N nPr Cl 5- SO₂Et 0.99 (t, 3H), 1.30 (t, 3H), 1.55 methoxymethyl- (s, 3H), 2.02 (m, 1H), 3.12 5-meth)-4,5- (d, 1H), 3.43 (q, 2H), 3.46 dihydro-1,2- (s, 3H), 3.48 (d, 1H), 3.55 oxazol-3-yl (q, 2H), 4.44 (t, 2H), 7.90 (d, 1H), 8.13 (d, 1H), 11.2 (br, s, 1H) 7-414 N nPr Cl SMe Me 10.08 (bs, 1H), 7.57 (d, 1H), 7.31 (d, 1H), 4.42 (t, 2H), 2.65 (s, 3H), 2.38 (s, 3H), 2.02 (sex, 2H), 0.99 (t, 3H) 7-415 N nPr Cl OCH₂cPr SO₂Me 9.80 (bs, 1H), 8.03 (d, 1H), 7.60 (d, 1H), 4.42 (t, 2H), 4.13 (d, 2H), 3.34 (s, 3H), 2.03 (quin, 2H), 1.44-1.52 (m, 1H), 1.00 (t, 3H), 0.67- 0.70 (m, 2H), 0.48-0.50 (m, 2H) 7-416 N nPr Cl OCH₂cPr SO₂Et 10.30 (bs, 1H), 8.01 (d, 1H), 7.58 (d, 1H), 4.43 (t, 2H), 4.11 (d, 2H), 3.53 (q, 2H), 2.04 (q, 2H), 1.44-1.70 (m, 1H), 1.28 (t, 3H), 1.00 (t, 3H), 0.66-0.71 (m, 2H), 0.46-0.50 (m, 2H) 7-417 N nPr Cl OCH₂cBu SO₂Me 10.20 (bs, 1H), 8.03 (d, 1H), 7.59 (d, 1H), 4.43 (t, 2H), 4.27 (d, 2H), 3.29 (s, 3H), 2.90-3.00 (m, 1H), 2.13- 2.22 (m, 2H), 1.96-2.07 (m, 6H), 1.00 (t, 3H) 7-418 N nPr Cl OCH₂cBu SO₂Et 10.00 (bs, 1H), 8.01 (d, 1H), 7.59 (d, 1H), 4.43 (t, 2H), 4.26 (d, 2H), 3.45 (q, 2H), 2.88-3.00 (m, 1H), 2.10- 2.22 (m, 2H), 1.96-2.07 (m, 6H), 1.27 (t, 3H), 1.00 (t, 3H) 7-419 N nPr Me O(CH₂)₂SMe Cl 11.43 (bs, 1H), 7.51 (d, 1H), 7.42 (d, 1H), 4.28 (t, 2H), 4.07 (t, 2H), 2.92 (t, 2H), 2.40 (s, 3H), 2.16 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-420 N nPr Me O(CH₂)₂SEt Cl 11.43 (bs, 1H), 7.51 (d, 1H), 7.42 (d, 1H), 4.28 (t, 2H), 4.05 (t, 2H), 2.95 (t, 2H), 2.63 (q, 2H), 2.40 (s, 3H), 1.88 (sex, 2H), 1.21 (t, 3H), 0.88 (t, 3H) 7-421 N nPr Me O(CH₂)₃SMe Cl 11.44 (bs, 1H), 7.51 (d, 1H), 7.41 (d, 1H), 4.28 (t, 2H), 3.98 (t, 2H), 2.71 (t, 2H), 2.37 (s, 3H), 2.09 (s, 3H), 2.05 (quin, 2H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-422 N nPr Me O(CH₂)₂SMe Br 11.42 (bs, 1H), 7.66 (d, 1H), 7.35 (d, 1H), 4.28 (t, 2H), 4.05 (t, 2H), 2.93 (t, 2H), 2.41 (s, 3H), 2.17 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-423 N nPr Me O(CH₂)₂SEt Br 11.43 (bs, 1H), 7.66 (d, 1H), 7.35 (d, 1H), 4.28 (t, 2H), 4.03 (t, 2H), 2.97 (t, 2H), 2.63 (q, 2H), 2.41 (s, 3H), 1.88 (sex, 2H), 1.22 (t, 3H), 0.88 (t, 3H) 7-424 N nPr Me O(CH₂)₃SMe Br 11.43 (bs, 1H), 7.65 (d, 1H), 7.34 (d, 1H), 4.28 (t, 2H), 3.96 (t, 2H), 2.72 (t, 2H), 2.38 (s, 3H), 2.09 (s, 3H), 2.08 (quin, 2H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-425 N n-Pr Me SEt Br 10.44 (bs, 1H), 7.69 (d, 1H), 7.51 (d, 1H), 4.40 (t, 2H), 2.88 (q, 2H), 2.81 (s, 3H), 2.03 (sex, 2H), 2.03 (s, 3H), 1.21 (t, 3H), 0.99 (t, 3H) 7-426 N nPr Cl OMe Cl 11.70 (bs, 1H), 7.68 (d, 1H), 7.53 (d, 1H), 4.31 (t, 2H), 3.88 (s, 3H), 3.31 (s, 3H), 1.89 (sex, 2H), 0.88 (t, 3H) 7-427 N nPr Cl O(CH₂)₂OMe Cl 11.70 (bs, 1H), 7.67 (d, 1H), 7.51 (d, 1H), 4.30 (t, 2H), 4.16-4.19 (m, 2H), 3.71- 3.73 (m, 2H), 3.31 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-428 N nPr Cl O(CH₂)₂SMe Cl 11.70 (bs, 1H), 7.68 (d, 1H), 7.52 (d, 1H), 4.31 (t, 2H), 4.19 (t, 2H), 2.94 (t, 2H), 2.16 (s, 3H), 1.89 (sex, 2H), 0.88 (t, 3H) 7-429 N nPr Cl O(CH₂)₂SEt Cl 11.60 (bs, 1H), 7.68 (d, 1H), 7.52 (d, 1H), 4.30 (t, 2H), 4.17 (t, 2H), 3.97 (t, 2H), 2.62 (q, 2H), 1.88 (sex, 2H), 1.21 (t, 3H), 0.88 (t, 3H) 7-430 N nPr Cl O(CH₂)₃SMe Cl 11.70 (bs, 1H), 7.68 (d, 1H), 7.51 (d, 1H), 4.30 (t, 2H), 4.12 (t, 2H), 2.72 (t, 2H), 2.09 (s, 3H), 2.07 (quin, 2H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-431 N nPr Cl OMe Br 11.70 (bs, 1H), 7.82 (d, 1H), 7.45 (d, 1H), 4.30 (t, 2H), 3.87 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-432 N nPr Cl OEt Br 11.69 (bs, 1H), 7.81 (d, 1H), 7.43 (d, 1H), 4.30 (t, 2H), 4.09 (q, 2H), 1.89 (sex, 2H), 1.42 (t, 3H), 0.88 (t, 3H) 7-433 N nPr Cl O(CH₂)₂OMe Br 11.70 (bs, 1H), 7.81 (d, 1H), 7.43 (d, 1H), 4.30 (t, 2H), 4.15-4.17 (m, 2H), 3.73- 3.75 (m, 2H), 3.34 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-434 N nPr Cl O(CH₂)₃OMe Br 11.70 (bs, 1H), 7.81 (d, 1H), 7.44 (d, 1H), 4.30 (t, 2H), 4.08 (t, 2H), 3.56 (t, 2H), 3.27 (s, 3H), 2.04 (quin, 2H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-435 N nPr Cl OCH₂(CO)NMe₂ Br 11.72 (bs, 1H), 7.82 (d, 1H), 7.47 (d, 1H), 4.72 (s, 3H), 4.30 (t, 2H), 3.02 (s, 3H), 2.88 (s, 3H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-436 N nPr Cl 1,4-dioxan-2- Br 11.70 (bs, 1H), 7.81 (d, 1H), ylmethoxy 7.45 (d, 1H), 4.30 (t, 2H), 3.89-4.07 (m, 4H), 3.77- 3.80 (m, 1H), 3.60-3.70 (m, 2H), 3.48-3.56 (m, 2H), 1.88 (sex, 2H), 0.88 (t, 3H) 7-437 N nPr Br O(CH₂)₃OMe Br 11.68 (bs, 1H), 7.84 (d, 1H), 7.39 (d, 1H), 4.32 (t, 2H), 4.06 (t, 2H), 3.57 (t, 2H), 3.28 (s, 3H), 2.06 (quin, 2H), 1.89 (sex, 2H), 0.88 (t, 3H) 7-438 N nPr Br O(CH₂)₂SMe Br 11.69 (bs, 1H), 7.85 (d, 1H), 7.40 (d, 1H), 4.32 (t, 2H), 4.17 (t, 2H), 2.97 (t, 2H), 2.18 (s, 3H), 1.89 (sex, 2H), 0.89 (t, 3H) 7-439 N nPr Br O(CH₂)₂SEt Br 11.68 (bs, 1H), 7.85 (d, 1H), 7.40 (d, 1H), 4.32 (t, 2H), 4.14 (t, 2H), 3.00 (t, 2H), 2.64 (q, 2H), 1.89 (sex, 2H), 1.22 (t, 3H), 0.88 (t, 3H) 7-440 N nPr Br O(CH₂)₃SMe Br 11.70 (bs, 1H), 7.84 (d, 1H), 7.40 (d, 1H), 4.32 (t, 2H), 4.09 (t, 2H), 2.73 (t, 2H), 2.09 (s, 3H), 2.09 (quin, 2H), 1.89 (sex, 2H), 0.88 (t, 3H) 7-441 N n-Pr F SOEt Cl 7-442 N n-Pr F SO₂Et Cl 7-443 N n-Pr F SEt CF₃ 7-444 N n-Pr F SOEt CF₃ 7-445 N n-Pr F SO₂Et CF₃ 7-446 N n-Pr Cl SCH₂c-Pr Cl 7-447 N n-Pr Cl SOCH₂c-Pr Cl 7-448 N n-Pr Cl SO₂CH₂c-Pr Cl 7-449 N nPr Cl O(CH₂)₂Cl SO₂Me 11.40 (bs, 1H), 8.03 (d, 1H), 7.61 (d, 1H), 4.58 (t, 2H), 4.45 (t, 2H), 3.98 (t, 2H), 2.02 (sex, 2H), 0.99 (t, 3H) 7-450 N nPr Cl O(CH₂)₂Cl SO₂Et 11.45 (bs, 1H), 8.01 (d, 1H), 7.61 (d, 1H), 4.57 (t, 2H), 4.45 (t, 2H), 3.96 (t, 2H), 3.51 (q, 2H), 2.01 (sex, 2H), 1.29 (t, 3H), 0.99 (t, 3H) 7-451 N n-Pr Cl SO₂Et Me 10.15 (bs, 1H), 7.18 (d, 1H), 7.56 (d, 1H), 4.40 (t, 2H), 3.49 (q, 2H), 2.85 (s, 3H), 2.02 (sex, 2H), 1.38 (t, 3H), 1.00 (t, 3H) 7-452 N n-Pr Cl SOEt Me 7.61 (d, 1H), 7.52 (d, 1H), 4.39 (t, 2H), 3.26-3.33 (m, 1H), 3.08-3.17 (m, 1H), 2.75 (s, 3H), 2.01 (sex, 2H), 1.39 (t, 3H), 1.00 (t, 3H) 7-453 N n-Pr Cl SO₂Me Me 10.10 (bs, 1H), 7.69 (d, 1H), 7.40 (d, 1H), 4.42 (t, 2H), 3.36 (s, 3H), 2.84 (s, 3H), 2.05 (sex, 2H), 0.99 (t, 3H) 7-454 N n-Pr Cl SOMe Me 10.60 (bs, 1H), 7.64 (d, 1H), 7.28 (d, 1H), 4.39 (t, 2H), 2.99 (s, 3H), 2.73 (s, 3H), 2.01 (sex, 2H), 0.99 (t, 3H)

TABLE 8 Compounds of the formula (I) according to the invention in which A represents N

Physical data No. B R X Z (¹H-NMR, DMSO-d₆, 400 MHz) 8-1 CH Me Cl Cl 8-2 N Me Cl Cl 8-3 CH Me Me Cl 8-4 N Me Me Cl 8.09 (d, 1H), 7.37 (d, 1H), 4.10 (s, 3H), 2.79 (s, 3H) 8-5 CH Me Cl SMe 8-6 N Me Cl SMe 11.83 (brs, 1H), 8.05 (d, 1H), 7.51 (d, 1H), 3.98 (s, 3H), 2.57 (s, 3H) 8-7 CH Me Me SO₂Me 8-8 N Me Me SO₂Me 8-9 CH Me Cl CF₃ 8.33 (d, 1H), 7.83 (s, 1H), 7.70 d, 1H), 3.84 (s, 3H) 8-10 N Me Cl CF₃ 8.41 (d, 1H), 7.83 (d, 1H), 4.13 (s, 3H) 8-11 CH Ph Cl CF₃ 8-12 N Ph Cl CF₃ 8.38 (d, 1H), 8.12 (d, 1H), 7.73- 7.49 (m, 5H) 8-13 N CH₂(CO)Me Cl CF3 8-14 N benzoyl Cl CF3 8-15 N allyl Cl CF3 8-16 N 4-Cl-benzyl Cl CF3 8-17 N CH₂CO₂Et Cl CF3 8-18 CH Me Me CF₃ 8-19 N Me Me CF₃ 8.33 (d, 1H), 7.73 (d, 1H), 4.13 (s, 3H), 2.86 (s, 3H) 8-20 CH Me CH₂OMe CF₃ 8-21 N Me CH₂OMe CF₃ 8.50 (d, 1H), 7.86 (d, 1H), 4.93 (s, 2H), 4.10 (s, 3H), 3.60 (s, 3H) 8-22 CH Me CH₂OC₂H₄OMe CF₃ 3.12 (s, 3H), 3.52 (m, 2H), 3.82 (m, 2H), 3.88 (s, 3H), 4.98 (s, 2H), 7.82 (s, 1H), 7.83 (d, 1H), 8.45 (d, 1H) 8-23 N Me CH₂OC₂H₄OMe CF₃ 3.12 (s, 3H), 3.52 (m, 2H), 3.80 (m, 2H), 4.08 (s, 3H), 5.0 (s, 2H), 7.85 (d, 1H), 8.43 (d, 1H) 8-24 N Me CH₂OEt CF₃ 1.31 (t, 3H), 3.83 (q, 2H), 4.11 (s, 3H), 4.97 (s, 2H), 7.86 (d, 1H), 8.52 (d, 1H), 11.47 (s, 1H) 8-25 N Me CH₂OiPr CF₃ 1.32 (d, 6H), 4.00 (m, 1H), 4.08 (s, 3H), 4.98 (s, 2H), 7.85 (d, 1H), 8.54 (d, 1H), 11.64 (s, 1H) 8-26 N Me CH₂OCH₂cPr CF₃ 0.24 (m, 2H), 0.53 (m, 2H), 1.09 (m, 1H), 3.55 (d, 2H), 4.10 (s, 3H), 5.00 (s, 2H), 7.84 (d, 1H), 8.50 (d, 1H), 11.52 (s, 1H) 8-27 N Me CH₂OCH₂CF₃ CF₃ 3.96 (q, 2H), 4.11 (s, 3H), 5.14 (s, 2H), 7.88 (d, 1H), 8.44 (d, 1H), 11.11 (s, 1H) 8-28 N Me CH₂OCH₂CH═CH₂ CF₃ 4.10 (s, 3H), 4.24 (d, 2H), 4.99 (s, 2H), 5.3 (dd, 2H), 5.93 (m, 1H), 7.85 (d, 1H), 8.48 (d, 1H), 11.23 (s, 1H) 8-29 N Me CH₂OCH₂CCH CF₃ 2.38 (t, 1H), 4.12 (s, 3H), 4.33 (d, 2H), 5.06 (s, 2H), 7.85 (d, 1H), 8.41 (d, 1H), 10.93 (s, 1H) 8-30 N Me CH₂SMe CF₃ 2.00 (s, 3H), 4.15 (s, 3H), 4.19 (s, 2H), 7.78 (d, 1H), 8.41 (d, 1H), 11.60 (s, 1H) 8-31 N Me CH₂SO₂Me CF₃ 2.96 (s, 3H), 3.87 (s, 3H), 5.45 (s, 2H), 7.72 (d, 1H), 8.91 (d, 1H) 8-32 N Me CH₂SEt CF₃ 1.40 (t, 3H), 2.40 (q, 2H), 3.97 (s, 3H), 4.19 (s, 2H), 7.71 (d, 1H), 8.41 (d, 1H) 8-33 N Me CH₂SO₂Et CF₃ 1.37 (t, 3H), 3.03 (q, 2H), 3.95 (s, 3H), 5.36 (s, 2H), 7.70 (d, 1H), 8.92 (d, 1H) 8-34 N Me Br CF₃ 12.07 (brs, 1H), 8.49 (d, 1H), 8.20 (d, 1H), 4.05 (s, 3H) 8-35 N Me SMe CF₃ 8.39 (d, 1H), 7.65 (d, 1H), 3.82 (s, 3H), 2.40 (s, 3H) 8-36 N Me SOMe CF₃ 8.67 (d, 1H), 8.24 (d, 1H), 3.99 (s, 3H), 2.89 (s, 3H) 8-37 N Me SO₂Me CF₃ 8.73 (d, 1H), 8.49 (d, 1H), 4.06 (s, 3H), 3.42 (s, 3H) 8-38 N Me F F 11.72 (brs, 1H), 8.59 (q, 1H), 7.71 (dd, 1H), 3.97 (s, 3H) 8-39 N Me SMe Cl 11.79 (brs, 1H), 8.22 (d, 1H), 7.46 (d, 1H), 3.95 (s, 3H), 2.47 (s, 3H) 8-40 N Me SO₂Me Cl 8.44 (d, 1H), 8.07 (d, 1H), 4.02 (s, 3H), 3.38 (s, 3H) 8-41 N Me Cl SO₂Me 12.09 (brs, 1H), 8.59 (d, 1H), 8.24 (d, 1H), 4.02 (s, 3H), 3.38 (s, 3H) 8-42 N Me SMe SMe 8-43 N Me SO₂Me SO₂Me 12.11 (brs, 1H), 8.75 (d, 1H), 8.51 (d, 1H), 4.05 (s, 3H), 3.47 (s, 6H) 8-44 N Et Me CF₃ 8.35 (d, 1H), 7.73 (d, 1H), 4.47 (q, 2H), 2.86 (s, 3H), 1.64 (t, 3H) 8-45 N Et CH₂OMe CF₃ 1.63 (t, 3H), 3.58 (s, 3H), 4.44 (q, 2H), 4.94 (s, 2H), 7.86 (d, 1H), 8.49 (d, 1H), 11.09 (s, 1H) 8-46 N Et CH₂OEt CF₃ 1.31 (t, 3H), 3.83 (q, 2H), 4.11 (s, 3H), 4.97 (s, 2H), 7.85 (d, 1H), 8.50 (d, 1H), 11.37 (s, 1H) 8-47 N Et CH₂OCH₂cPr CF₃ 0.24 (m, 2H), 0.54 (m, 2H), 1.11 (m, 1H), 1.62 (t, 3H), 3.59 (d, 2H), 4.44 (q, 2H), 5.00 (s, 2H), 7.85 (d, 1H), 8.53 (d, 1H), 11.41 (s, 1H) 8-48 N Et CH₂OCH₂CF₃ CF₃ 1.51 (t, 3H), 3.89 (q, 2H), 4.32 (q, 2H), 5.18 (s, 2H), 7.66 (d, 1H), 8.44 (d, 1H) 8-49 N Et CH₂OC₃H₆OMe CF₃ 1.63 (t, 3H), 1.91 (m, 2H), 3.12 (s, 3H), 3.42 (m, 2H), 3.84 (m, 2H), 4.43 (q, 2H), 4.95 (s, 2H), 7.85 (d, 1H), 8.48 (d, 1H), 11.12 (s, 1H) 8-50 N Et CH₂OCH₂CH═CH₂ CF₃ 1.62 (t, 3H), 4.24 (d, 2H), 4.43 (q, 2H), 4.99 (s, 2H), 5.3 (dd, 2H), 5.93 (m, 1H), 7.85 (d, 1H), 8.48 (d, 1H), 11.13 (s, 1H) 8-51 N Et CH₂OCH₂CCH CF₃ 1.63 (t, 3H), 2.39 (t, 1H), 4.35 (d, 2H), 4.44 (q, 2H), 5.06 (s, 2H), 7.85 (d, 1H), 8.43 (d, 1H), 10.75 (s, 1H) 8-52 N CH₂(CO)Me Cl CF₃ 12.11 (s, 1H), 8.47 (d, 1H), 8.18 (d, 1H), 5.59 (s, 2H), 2.26 (s, 3H) 8-53 N 4-Cl-benzyl Cl CF₃ 12.08 (s, 1H), 8.48 (d, 1H), 8.18 (d, 1H), 7.48 (d, 2H), 7.34 (d, 2H), 5.65 (s, 2H) 8-54 N CH₂CO₂Et Cl CF₃ 12.23 (s, 1H), 8.50 (d, 1H), 8.19 (d, 1H), 5.48 (s, 2H), 4.20 (q, 2H), 1.21 (t, 3H) 8-55 N Et Cl CF₃ 8.36 (d, 1H), 7.82 (d, 1H), 4.48 (q, 2H), 1.64 (t, 3H) 8-56 N Et Br CF₃ 11.97 (brs, 1H), 8.50 (d, 1H), 8.20 (d, 1H), 4.41 (q, 2H), 1.50 (t, 3H) 8-57 N Et F F 11.61 (brs, 1H), 8.60 (q, 1H), 7.40 (dd, 1H), 4.33 (q, 2H), 1.45 (t, 3H) 8-58 N Et Me Cl 8.10 (d, 1H), 7.42 (d, 1H), 4.22 (q, 2H), 2.63 (s, 3H), 1.39 (t, 3H) 8-59 N nPr Me CF₃ 8.26 (d, 1H), 7.72 (d, 1H), 4.40 (t, 2H), 2.85 (s, 3H), 2.04 (m, 2H), 1.01 (t, 3H) 8-60 N nPr Cl CF₃ 8.38 (d, 1H), 7.81 (d, 1H), 4.39 (t, 2H), 2.04 (m, 2H), 1.01 (t, 3H) 8-61 N nPr Me Cl 7.60 (d, 1H), 7.26 (d, 1H), 4.39 (t, 2H), 2.52 (s, 3H), 1.98 (m, 2H), 0.98 (t, 3H) 8-62 N nPr CH₂OMe CF₃ 0.99 (t, 3H), 2.03 (q, 2H), 3.56 (s, 3H), 4.36 (t, 2H), 4.94 (s, 2H), 7.86 (d, 1H), 8.48 (d, 1H), 11.17 (s, 1H) 8-63 N nPr CH₂OEt CF₃ 1.00 (t, 3H), 1.29 (t, 3H), 2.03 (m, 2H), 3.80 (q, 2H), 4.37 (q, 2H), 4.97 (s, 2H), 7.85 (d, 1H), 8.50 (d, 1H), 11.36 (s, 1H) 8-64 N nPr CH₂OCH₂CF₃ CF₃ 0.99 (t, 3H), 2.03 (m, 2H), 3.94 (q, 2H), 4.37 (t, 2H), 5.12 (s, 2H), 7.86 (d, 1H), 8.43 (d, 1H), 11.30 (s, 1H) 8-65 N nPr CH₂OCH₂CCH CF₃ 0.96 (t, 3H), 1.92 (m, 2H), 2.32 (t, 1H), 4.16 (d, 2H), 4.25 (t, 2H), 5.14 (s, 2H), 7.65 (d, 1H), 8.40 (d, 1H) 8-66 N nPr CH₂OCH₂CH═CH₂ CF₃ 0.99 (t, 3H), 2.03 (m, 2H), 4.24 (d, 2H), 4.35 (t, 2H), 4.98 (s, 2H), 5.3 (dd, 2H), 5.93 (m, 1H), 7.85 (d, 1H), 8.49 (d, 1H), 11.11 (s, 1H) 8-67 N nPr CH₂(3-methyl-2- CF₃ 2.55 (s, 3H), 3.19 (m, 4H), 3.87 oxoimidazolidin-1- (s, 3H), 4.64 (s, 2H), 7.62 (d, 1H), yl) 8.01 (d, 1H), 13.3 (s, 1H) 8-68 N Me iPr CF₃ 8-69 N Me CH₂ ₍3-methyl-2- CF₃ 2.55 (s, 3H), 3.19 (m, 4H), 3.87 oxoimidazolidin-1- (s, 3H), 4.64 (s, 2H), 7.62 (d, 1H), yl) 8.01 (d, 1H), 13.3 (br, s, 1H) 8-70 CH Me CH₂(3-methyl-2- CF₃ oxoimidazolidin-1- yl) 8-71 CH M e CH₂OC₃H₆OMe CF₃ 1.89 (m, 2H), 3.14 (s, 3H), 3.40 (t, 2H), 3.78 (t, 2H), 3.88 (s, 3H), 3.95 (s, 2H), 7.80 (s, 1H), 7.80 (d, 1H), 8.45 (d, 1H), 10.7 (br, s, 1H) 8-72 N Me CH₂OC₃H₆OMe CF₃ 8-73 CH Me CH₂SMe CF₃ 2.06 (s, 3H), 3.89 (s, 3H), 4.25 (s, 2H), 7.63 (s, 1H), 7.63 (d, 1H), 8.32 (d, 1H), 10.5 (br, s, 1H 8-74 CH Me CH₂CO₂Me CF₃ 8-75 N Et CH₂OC₂H₄OMe CF₃ 8-76 N Me Me 3-me- 1,2,4- triazol-1- yl 8-77 N allyl CH₂OMe CF₃ 8-78 N Ph Me CF₃ 12.00 (s, 1H), 8.22 (d, 1H), 7.89 (d, 1H), 7.72-7.69 (m, 2H), 7.66- 7.59 (m, 3H), 2.44 (s, 3H) 8-79 N nPr CH₂OC₂H₄OMe CF₃ 8-80 N allyl CH₂(1,1- CF₃ 11.90 (s, 1H), 8.37 (d, 1H), 8.09 dioxoisothiazolidin- (d, 1H), 6.08-6.02 (m, 1H), 5.33 2-yl) (d, 1H), 5.27 (d, 1H), 4.51 (s, 2H), 3.26-3.21 (m, 4 H), 2.25-2.20 (m, 2H) 8-81 N Me CH₂OMe SO₂Me 8-82 N Me CH₂OC₂H₄OMe SO₂Me

B. Formulation Examples

-   a) A dust is obtained by mixing 10 parts by weight of a compound of     the formula (I) and/or a salt thereof and 90 parts by weight of talc     as inert substance and comminuting the mixture in a hammer mill. -   b) A wettable powder which is readily dispersible in water is     obtained by mixing 25 parts by weight of a compound of the     formula (I) and/or a salt thereof, 64 parts by weight of     kaolin-containing quartz as inert substance, 10 parts by weight of     potassium lignosulfonate and 1 part by weight of sodium     oleoylmethyltaurinate as wetting agent and dispersant, and grinding     the mixture in a pinned-disk mill. -   c) A readily water-dispersible dispersion concentrate is obtained by     mixing 20 parts by weight of a compound of the formula (I) and/or a     salt thereof with 6 parts by weight of alkylphenol polyglycol ether     (®Triton X 207), 3 parts by weight of isotridecanol polyglycol ether     (8 EO) and 71 parts by weight of paraffinic mineral oil (boiling     range for example about 255 to above 277° C.) and grinding the     mixture in a ball mill to a fineness of below 5 microns. -   d) An emulsifiable concentrate is obtained from 15 parts by weight     of a compound of the formula (I) and/or a salt thereof, 75 parts by     weight of cyclohexanone as solvent and 10 parts by weight of     oxethylated nonylphenol as emulsifier. -   e) Water-dispersible granules are obtained by mixing     -   75 parts by weight of a compound of the formula (I) and/or a         salt thereof,     -   10 parts by weight of calcium lignosulfonate,     -   5 parts by weight of sodium lauryl sulfate,     -   3 parts by weight of polyvinyl alcohol and     -   7 parts by weight of kaolin,     -   grinding the mixture in a pinned-disk mill, and granulating the         powder in a fluidized bed by spraying on water as granulating         liquid. -   f) Water-dispersible granules are also obtained by homogenizing and     precomminuting, in a colloid mill,     -   25 parts by weight of a compound of the formula (I) and/or a         salt thereof,     -   5 parts by weight of sodium         2,2′-dinaphthylmethane-6,6′-disulfonate,     -   2 parts by weight of sodium oleoylmethyltaurinate,     -   1 part by weight of polyvinyl alcohol,     -   17 parts by weight of calcium carbonate and     -   50 parts by weight of water,     -   subsequently grinding the mixture in a bead mill and atomizing         and drying the resulting suspension in a spray tower by means of         a single-substance nozzle.

C. Biological Examples 1. Pre-Emergence Herbicidal Action Against Harmful Plants

Seeds of monocotyledonous or dicotyledonous weed plants or crop plants are planted in wood-fiber pots in sandy loam and covered with soil. The compounds according to the invention, formulated in the form of wettable powders (WP) or emulsion concentrates (EC), are then applied as aqueous suspension or emulsion at a water application rate of 600 to 800 l/ha (converted) with the addition of 0.2% of wetting agent to the surface of the covering soil. After the treatment, the pots are placed in a greenhouse and kept under good growth conditions for the test plants. The visual assessment of the damage to the test plants is carried out after a trial period of 3 weeks by comparison with untreated controls (herbicidal activity in percent (%): 100% activity=the plants have died, 0% activity=like control plants). Here, for example, the compounds Nos. 1-124, 1-148, 1-149, 1-205, 1-229, 1-247, 1-249, 1-258, 1-279, 1-286, 1-503, 1-556, 2-148, 4-8, 4-9, 4-10, 4-26, 4-124, 4-138, 4-144, 4-221, 4-260, 4-410, 4-450, 4-501, 4-652, 4-686, 4-718, 5-122, 5-156, 5-164, 5-210, 5-276, 5-432, 5-510, 5-597, 5-676, 7-17, 7-30, 7-37, 7-124, 7-180, 7-218, 7-318, 7-732, 8-2, 8-10, 8-34 and 8-79 each show, at an application rate of 80 g/ha, an activity of at least 80% against Echinocloa crus galli and Veronica persica. The compounds Nos. 1-124, 1-148, 1-149, 1-205, 1-249, 1-258, 1-260, 1-536, 1-549, 1-550, 1-556, 2-148, 4-9, 4-10, 4-13, 4-80, 4-125, 4-144, 4-193, 4-219, 4-260, 4-287, 4-411, 4-460, 4-532, 4-632, 4-664, 4-769, 4-874, 4-902, 5-119, 5-121, 5-166, 5-231, 5-281, 5-423, 5-456, 5-636, 5-636, 5-636, 5-713, 5-800, 6-148, 6-149, 6-189, 6-475, 7-24, 7-30, 7-37, 7-55, 7-106, 7-173, 7-299, 7-329, 7-413, 8-4, 8-10, 8-34, 8-66, 8-77 and 8-79 each show, at an application rate of 80 g/ha, an activity of at least 80% against Abutilon theophrasti and Amaranthus retroflexus. The compounds Nos. 1-124, 1-148, 1-205, 1-249, 1-258, 1-267, 1-286, 1-536, 1-555, 2-148, 4-8, 4-25, 4-108, 4-125, 4-144, 4-148, 4-198, 4-260, 4-314, 4-411, 4-467, 4-538, 4-718, 4-892, 5-124, 5-166, 5-242, 5-392, 5-414, 5-598, 5-614, 5-728, 6-148, 6-149, 6-189, 7-24, 7-30, 7-37, 7-179, 7-213, 7-310, 7-411, 8-10, 8-24, 8-75, 8-79 and 8-80 each show, at an application rate of 80 g/ha, an activity of at least 80% against Matricaria inodora and Veronica persica.

2. Post-Emergence Herbicidal Action Against Harmful Plants

Seeds of monocotyledonous and dicotyledonous weed and crop plants are placed in sandy loam in wood-fiber pots, covered with soil and cultivated in a greenhouse under good growth conditions. 2 to 3 weeks after sowing, the test plants are treated at the one-leaf stage. The compounds according to the invention, formulated in the form of wettable powders (WP) or emulsion concentrates (EC), are then sprayed as aqueous suspension or emulsion at a water application rate of 600 to 800 l/ha (converted) with the addition of 0.2% of wetting agent onto the green parts of the plants. After the test plants have been kept in the greenhouse under optimum growth conditions for about 3 weeks, the activity of the preparations is rated visually in comparison to untreated controls (herbicidal activity in percent (%): 100% activity=the plants have died, 0% activity=like control plants). Here, for example, the compounds Nos. 1-16, 1-148, 1-188, 1-205, 1-249, 1-258, 1-267, 1-313, 1-315, 1-468, 1-504, 1-602, 2-148, 4-10, 4-96, 4-119, 4-144, 4-148, 4-260, 4-315, 4-414, 4-504, 4-604, 4-712, 4-839, 4-900, 5-67, 5-150, 5-203, 5-383, 5-413, 5-532, 5-653, 5-712, 5-802, 6-149, 6-238, 6-475, 7-30, 7-100, 7-216, 7-325, 7-411, 8-9, 8-10, 8-55, 8-64, 8-79 and 8-79 each show, at an application rate of 80 g/ha, an activity of at least 80% against Amaranthus retroflexus and Viola tricolor. The compounds Nos. 1-16, 1-148, 1-188, 1-249, 1-258, 1-267, 1-272, 1-313, 1-468, 1-537, 1-605, 2-148, 4-10, 4-96, 4-119, 4-144, 4-148, 4-260, 4-365, 4-414, 4-534, 4-623, 4-719, 4-839, 4-900, 5-31, 5-122, 5-206, 5-386, 5-437, 5-586, 5-629, 5-716, 5-802, 6-148, 6-149, 6-189, 6-238, 6-294, 6-475, 7-30, 7-37, 7-127, 7-215, 7-321, 7-412, 8-9, 8-10, 8-22, 8-46, 8-59, 8-69, 8-77 and 8-79 each show, at an application rate of 80 g/ha, an activity of at least 80% against Abutilon theophrasti and Veronica persica. 

1. A compound comprising an N-(tetrazol-4-yl)- or N-(triazol-3-yl)arylcarboxamide of formula (I) and/or a salt thereof

in which A represents N or CY, B represents N or CH, X represents nitro, halogen, cyano, formyl, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, C(O)NR¹OR¹, OR¹, OCOR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², NR₁R₂, P(O)(OR⁵)₂, CH₂P(O)(OR⁵)₂, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups, Y represents hydrogen, nitro, halogen, cyano, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, CO(NOR¹)R¹, NR¹SO₂R², NR¹COR¹, OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂ (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO2R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-CN, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², N(R¹)₂, P(O)(OR⁵)₂, CH₂P(O)(OR⁵)₂, (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups, Z represents halogen, cyano, thiocyanato, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, OCOOR¹, NR¹COOR¹, C(O)N(R¹)₂, NR¹C(O)N(R¹)₂, OC(O)N(R¹)₂, C(O)NR¹OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², N(R¹)₂, P(O)(OR⁵)₂, heteroaryl, heterocyclyl or phenyl, where the three last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy and halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups, or Z may also represent hydrogen, (C₁-C₆)-alkyl or (C₁-C₆)-alkoxy if Y represents the radical S(O)_(n)R², R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₂-C₆)-alkynyl, CH₂R⁶, heteroaryl, heterocyclyl or phenyl, where the three last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl, R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-haloalkenyl, (C₂-C₆)-alkynyl, (C₂-C₆)-haloalkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, (C₃-C₆)-halocycloalkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocycl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl, (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 21 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, thiocyanato, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR³, OCOR³, SCOR⁴, NR³COR³, NR³SO₂R⁴, CO₂R³, COSR⁴, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups, R² represents (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-haloalkenyl, (C₂-C₆)-alkynyl, (C₂-C₆)-haloalkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, (C₃-C₆)-halocycloalkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl, (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 21 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, thiocyanato, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR³, OCOR³, SCOR⁴, NR³COR³, NR³SO₂R⁴, CO₂R³, COSR⁴, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups, R³ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl or (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, R⁴ represents (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl, R⁵ represents methyl or ethyl, R⁶ represents acetoxy, acetamido, N-methylacetamido, benzoyloxy, benzamido, N-methylbenzamido, methoxycarbonyl, ethoxycarbonyl, benzoyl, methylcarbonyl, piperidinylcarbonyl, morpholinylcarbonyl, trifluoromethylcarbonyl, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, (C₁-C₆)-alkoxy, (C₃-C₆)-cycloalkyl or represents heteroaryl, heterocyclyl or phenyl, each of which is substituted by s radicals from the group consisting of methyl, ethyl, methoxy, trifluoromethyl and halogen, n represents 0, 1 or 2, s represents 0, 1, 2 or 3, with the proviso that X and Z both do not represent chlorine and B does not represent nitrogen if R represents n-propyl.
 2. The compound as claimed in claim 1 in which A represents N or CY, B represents N or CH, X represents nitro, halogen, cyano, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, OR¹, OCOR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹ or (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups, Y represents hydrogen, nitro, halogen, cyano, thiocyanato, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkenyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, OR¹, COOR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂ N(R¹)₂, N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups, Z represents halogen, cyano, thiocyanato, halo-(C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, halo-(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, halo-(C₃-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, halo-(C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, halo-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, COR¹, COOR¹, C(O)N(R¹)₂, C(O)NR¹OR¹, OSO₂R², S(O)_(n)R², SO₂OR¹, SO₂N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-OCOR¹, (C₁-C₆)-alkyl-OSO₂R², (C₁-C₆)-alkyl-CO₂R¹, (C₁-C₆)-alkyl-SO₂OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², 1,2,4-triazol-1-yl, or Z may also represent hydrogen, (C₁-C₆)-alkyl or (C₁-C₆)-alkoxy if Y represents the radical S(O)_(n)R², R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₃-C₇)-cycloalkylmethyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, acetylmethyl, methoxymethyl, or represents phenyl or benzyl which are substituted by s radicals from the group consisting of methyl, methoxy, trifluoromethyl and halogen, R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 16 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR^(S), OCOR³, NR³COR³, NR³SO₂R⁴, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups, R² represents (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C1-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C1-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where these radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, NR³SO₂R⁴, COR³, OCOR³, NR³COR³, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups, R³ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl or (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, R⁴ represents (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl, n represents 0, 1 or 2, s represents 0, 1, 2 or
 3. 3. The compound as claimed in claim 1 in which A represents N or CY, B represents N or CH, X represents nitro, halogen, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, OR¹, S(O)_(n)R², (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, where the two last-mentioned radicals are each substituted by s radicals halogen, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, and where heterocyclyl carries 0 to 2 oxo groups, Y represents hydrogen, nitro, halogen, cyano, (C₁-C₆)-alkyl, (C₁-C₆)-haloalkyl, OR¹, S(O)_(n)R², SO₂N(R¹)₂, N(R¹)₂, NR¹SO₂R², NR¹COR¹, (C₁-C₆)-alkyl-S(O)_(n)R², (C₁-C₆)-alkyl-OR¹, (C₁-C₆)-alkyl-CON(R¹)₂, (C₁-C₆)-alkyl-SO₂N(R¹)₂, (C₁-C₆)-alkyl-NR¹COR¹, (C₁-C₆)-alkyl-NR¹SO₂R², (C₁-C₆)-alkyl-phenyl, (C₁-C₆)-alkyl-heteroaryl, (C₁-C₆)-alkyl-heterocyclyl, phenyl, heteroaryl or heterocyclyl, where the 6 last-mentioned radicals are each substituted by s radicals from the group consisting of halogen, nitro, cyano, (C₁-C₆)-alkyl, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)—(C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, halo-(C₁-C₆)-alkoxy, (C₁-C₆)-alkoxy-(C₁-C₄)-alkyl and cyanomethyl, and where heterocyclyl carries 0 to 2 oxo groups, Z represents halogen, cyano, halo-(C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl, S(O)_(n)R², 1,2,4-triazol-1-yl, or Z may also represent hydrogen, methyl, methoxy or ethoxy if Y represents the radical S(O)_(n)R², R represents (C₁-C₆)-alkyl, (C₃-C₇)-cycloalkyl, halo-(C₁-C₆)-alkyl, (C₃-C₇)-cycloalkylmethyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, acetylmethyl or methoxymethyl, or represents phenyl which is substituted by s radicals from the group consisting of methyl, methoxy, trifluoromethyl and halogen; R¹ represents hydrogen, (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₆)-alkyl-O—(C₁-C₆)-alkyl, phenyl, phenyl-(C₁-C₆)-alkyl, heteroaryl, (C₁-C₆)-alkyl-heteroaryl, heterocyclyl, (C₁-C₆)-alkyl-heterocyclyl, (C₁-C₆)-alkyl-O-heteroaryl, (C₁-C₆)-alkyl-O-heterocyclyl, (C₁-C₆)-alkyl-NR³-heteroaryl or (C₁-C₆)-alkyl-NR³-heterocyclyl, where the 16 last-mentioned radicals are substituted by s radicals from the group consisting of cyano, halogen, nitro, OR³, S(O)_(n)R⁴, N(R³)₂, NR³OR³, COR³, OCOR³, NR³COR³, NR³SO₂R⁴, CO₂R³, CON(R³)₂ and (C₁-C₄)-alkoxy-(C₂-C₆)-alkoxycarbonyl, and where heterocyclyl carries 0 to 2 oxo groups, R² represents (C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl or (C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, where the three radicals mentioned above are each substituted by s radicals from the group consisting of halogen and OR³, R³ represents hydrogen or (C₁-C₆)-alkyl, R⁴ represents (C₁-C₆)-alkyl, n represents 0, 1 or 2, s represents 0, 1, 2 or
 3. 4. A herbicidal composition which comprises a herbicidally effective amount of at least one compound as claimed in claim
 1. 5. The herbicidal composition as claimed in claim 4 in a mixture with one or more formulation auxiliaries.
 6. The herbicidal composition as claimed in claim 4, comprising at least one further pesticidally active compound selected from the group consisting of insecticides, acaricides, herbicides, fungicides, safeners, and growth regulators.
 7. The herbicidal composition as claimed in claim 4, comprising a safener.
 8. The herbicidal composition as claimed in claim 4, comprising at least one of cyprosulfamid, cloquintocet-mexyl, mefenpyr-diethyl or isoxadifen-ethyl.
 9. The herbicidal composition as claimed in claim 4, comprising a further herbicide.
 10. A method for controlling unwanted plants comprising applying an effective amount of at least one compound as claimed in claim 1 to plants and/or a site of unwanted vegetation.
 11. A method of using a compound as claimed in claim 1 comprising using said compound for controlling unwanted plants.
 12. The method as claimed in claim 11 wherein the compound is used for controlling unwanted plants in crops of useful plants.
 13. The method as claimed in claim 12 wherein the useful plants are transgenic useful plants. 